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Thursday 22 January 2015

Prof. Floris Rutjes

Floris Rutjes, Professor, Radboud University Nijmegen, Netherlands

Professor in Synthetic Organic Chemistry

Director Educational Institute for Molecular Sciences

Floris Rutjes is full professor in organic synthesis at Radboud University Nijmegen. His research interests comprise the application of catalysis in the synthesis of biologically relevant molecules, and synthesis in microreactors.

He has received several awards including the Gold Medal of the Royal Netherlands Chemical Society (KNCV, 2002) and the AstraZeneca award for research in organic chemistry (2003).

He is co-founder of the companies Chiralix and FutureChemistry, and in 2008 received the award of ‘Most entrepreneurial scientist of the Netherlands 2008’.

Currently, he is also Director of the Educational Institute for Molecular Sciences at Radboud University Nijmegen.

His research interests comprise the application of catalysis in the synthesis of biologically relevant molecules and natural products, the development of new molecular diagnostic tools for application in life sciences, and synthesis in microreactors.

links

EMAIL f.rutjes@science.ru.nl
https://twitter.com/florisrutjes,,@Florisrutges

http://www.soc.science.ru.nl/
facebook https://m2.facebook.com/floris.rutjes.7

linkedin nl.linkedin.com/pub/floris-rutjes/5/b32/117

At flow chemistry conference mumbai, india 22 jan 2015

Rutjes, Prof. F.P.J.T. (Floris)

Synthetic Organic Chemistry, professor

Chair:	Synthetic Organic Chemistry
Faculty:	Faculty of Science
E-Mail:	f.rutjes@science.ru.nl
Telephone:	024-3653202
Visiting Address:	Interne adressering: 50 Heyendaalseweg 135 6525 AJ Nijmegen
Postal Address:	Postbus 9010 6500 GL Nijmegen

Institute for Molecular Sciences, director of education

Visiting Address:

Interne adressering: 52
Heyendaalseweg 135
6525 AJ Nijmegen

Experience

Professor in Synthetic Organic Chemistry

Radboud University Nijmegen

1999 – Present

Assistant professor

University of Amsterdam

January 1996 – October 1999 (3 years 10 months)

Post-doctoral fellow

The Scripps Research Institute

July 1993 – March 1995 (1 year 9 months)

Education

University of Amsterdam

PhD, Organic Synthesis

1988 – 1993

PLACE LIVED

Nijmegen, Netherlands

Current City

Heiloo

Hometown

REALTIONSHIP

Miranda Teerhuis, married

Heyendaal castle (now serving as the Faculty Club of the university) is of old the center of Heyendaal estate, where later on most Radboud University buildings have been established.

City of Nijmegen

Whether the reason for your stay in Nijmegen is to study, to work or to perform research at the university, there is a lot more to the city of Nijmegen than just the university. In your free time there are plenty of different things you can do to enjoy yourself. Whether you prefer shopping, going to a museum or to a movie, it is all possible in this city. Here you will find a listing of shopping areas, museums and movie theatres, as well as information on the Tourist Information Office.

Apart from information on culture, we also provide you with some background information on the history of Nijmegen and some interesting links. We hope you will enjoy spending time in the city of Nijmegen.

Radboud University Nijmegen
Radboud University is located in the oldest city in the Netherlands - Nijmegen. The city dates from Roman times when its name was Noviomagus or New Market. Today, it has some 165,000 inhabitants and is a safe and friendly place with a rich social and cultural life.

Situated close to the German border, Nijmegen lies on the banks of the River Waal, a branch of the Rhine. A recent survey found that local people regard students as enriching their city and find them friendly and lively. The students themselves appreciate the green surroundings and the many opportunities that the city offers for relaxation and entertainment.

Rutjes, Prof. F.P.J.T. (Floris)

Keywords:

organic synthesis, combinatorial chemistry, medicines

Expertise
Professor Floris Rutjes researches new routes for the synthesis of organic molecules with specific biological properties. His group focuses both on new molecules and on improving existing routes using biocatalysis.

Professor Rutjes also develops microreactors. These are miniature systems in which the reaction channel has a diameter of 10 to 500 micrometers. Microreactors can be used for example in the optimization of chemical reactions, as well as in the simultaneous production of large numbers of substances. This allows his research group, for example, to make certain sizes of biological active molecules. The interactions of these new molecules with components in the cell are studied within the life sciences.

The research carried out by Professor Rutjes is important in the development of new drugs. Knowledge from the group is transferred to the pharmaceuticals industry through the spin-off company Chiralix.

Publications in Metis

Scientific publications:

Steendam, R.R.E., Brouwer, M.C.T., Huijs, E.M.E., Kulka, M.W., Meekes, H., Enckevort, W.J.P. van, Raap, J., Rutjes, F.P.J.T. & Vlieg, E. (2014). Enantiopure isoindolinones through viedma ripening. Chemistry-a European Journal, 20(42), 13527-13530. 10.1002/chem.201404320
Wammes, A.E.M., Hendriks, T.G., Amatdjais-Groenen, H.I.V., Wijdeven, M.A., Hest, J.C.M. van, Delft, F.L. van, Ritschel, T. & Rutjes, F.P.J.T. (2014). Influence of azide incorporation on binding affinity by small papain inhibitors. Bioorganic & Medicinal Chemistry, 22(20), 5593-5603. 10.1016/j.bmc.2014.06.001
Irfan, M., Eshuis, N., Spannring, P., Tessari, M., Feiters, M.C. & Rutjes, F.P.J.T. (2014).Liquid-phase parahydrogen-induced polarization (phip) with ligand-capped platinum nanoparticles. Journal of Physical Chemistry C, 118(24), 13313-13319. 10.1021/jp504698w
Oers, M.C.M. van, Rutjes, F.P.J.T. & Hest, J.C.M. van (2014). Cascade reactions in nanoreactors. Curr Opin Biotechnol, 28, 10-16. 10.1016/j.copbio.2013.10.011
Debets, M.F., Prins, J.S., Merkx, D., Berkel, S.S. van, Delft, F.L. van, Hest, J.C.M. van & Rutjes, F.P.J.T. (2014). Synthesis of dibac analogues with excellent spaac rate constants.Organic & Biomolecular Chemistry, 12(27), 5031-5037. 10.1039/c4ob00694a
Eshuis, N., Hermkens, N., Weerdenburg, B.J.A. van, Feiters, M.C., Rutjes, F.P.J.T., Wijmenga, S.S. & Tessari, M. (2014). Toward nanomolar detection by nmr through sabre hyperpolarization. Journal of the American Chemical Society, 136(7), 2695-2698.
Pijl, F. van der, Harmel, R.K., Richelle, G.J.J., Janssen, P., Delft, F.L. van & Rutjes, F.P.J.T. (2014). Organocatalytic entry into 2,6-disubstituted aza-achmatowicz piperidinones: Application to (-)-sedacryptine and its epimer. Organic Letters, 16(7), 2038-2041.
Ritzen, B., Richelle, G.J.J., Brocken, L., Delft, F.L. van & Rutjes, F.P.J.T. (2014). Enzyme and gold catalysis: A new enantioselective entry into functionalized 4-hydroxy-2-pyrrolines. Synlett, 25(2), 270-274.
Lenstra, D.C., Rutjes, F.P.J.T. & Mecinovic, J. (2014). Triphenylphosphine-catalysed amide bond formation between carboxylic acids and amines. Chemical Communications, 50(43), 5763-5766.
Willemsen, J.S., Megens, R.P., Roelfes, G., Hest, J.C.M. van & Rutjes, F.P.J.T. (2014). A one-pot oxidation/enantioselective oxa-michael cascade. European Journal of Organic Chemistry, 2014(14), 2892-2898.
Oers, M.C.M. van, Abdelmohsen, L.K.E.A., Rutjes, F.P.J.T. & Hest, J.C.M. van (2014). Aqueous asymmetric cyclopropanation reactions in polymersome membranes. Chemical Communications, 50(31), 4040-4043.
Brauch, S., Wang, Z.P., Oers, M.C.M. van, Hest, J.C.M. van & Rutjes, F.P.J.T. (2014). Supramolecular chemical reactors towards the application of self-assembled polymersomes in cascade reactions. Chimica Oggi-Chemistry Today, 32(3), 73-77.
Kalkeren, H.A. van, Grotenhuis, C. te, Haasjes, F.S., Hommersom, C.A., Rutjes, F.P.J.T. & Delft, F.L. van (2013). Catalytic staudinger/aza-wittig sequence by in situ phosphane oxide reduction. European Journal of Organic Chemistry, 2013(31), 7059-7066.
Jansen, P.A.M., Diepen, J.A. van, Ritzen, B., Zeeuwen, P.L.J.M., Cacciatore, I., Cornacchia, C., Vlijmen-Willems, I.M. van, Heuvel, E. de, Botman, P.N.M., Blaauw, R.H., Hermkens, P.H.H., Rutjes, F.P.J.T. & Schalkwijk, J. (2013). Discovery of small molecule vanin inhibitors: new tools to study metabolism and disease. ACS Chemical Biology, 8(3), 530-4.
Rachwalski, M., Vermue, N. & Rutjes, F.P.J.T. (2013). Recent advances in enzymatic and chemical deracemisation of racemic compounds. Chemical Society Reviews, 42(24), 9268-9282.
Blanco-Ania, D., Aben, R.W.M., Berkom, L.W.A. van, Scheeren, H.W. & Rutjes, F.P.J.T. (2013). High-pressure-mediated extension of the privileged steroid scaffold. European Journal of Organic Chemistry, n/a-n/a.
Kalkeren, H.A. van, Delft, F.L. van & Rutjes, F.P.J.T. (2013). Organophosphorus Catalysis to Bypass Phosphine Oxide Waste. Chemsuschem, 6(9), 1615-1624. http://dx.doi.org/10.1002/cssc.201300368
Gool, J.J.F. van, Broek, S.A.M.W. van den, Ripken, R.M., Nieuwland, P.J., Koch, K. & Rutjes, F.P.J.T. (2013). Highly Controlled Gas/Liquid Processes in a Continuous Lab-Scale Device. Chemical Engineering & Technology, 36(6), 1042-1046. http://dx.doi.org/10.1002/ceat.201200553
Rachwalski, M., Leenders, T., Kaczmarczyk, S., Kielbasinski, P., Lesniak, S. & Rutjes, F.P.J.T. (2013). Efficient catalysts for asymmetric Mannich reactions. Organic & Biomolecular Chemistry, 11(25), 4207-4213. http://dx.doi.org/10.1039/c3ob40681d
Boltje, T.J., Heise, T., Rutjes, F.P.J.T. & Delft, F.L. van (2013). A Divergent Method to Prepare 5-Amino-, 5-N-Acetamido-, and 5-N-Glycolylsialosides. European Journal of Organic Chemistry, 2013(24), 5257-5261. http://dx.doi.org/10.1002/ejoc.201300664
Weerdenburg, B.J.A. van, Gloggler, S., Eshuis, N., Engwerda, A.H.J., Smits, J.M.M., Gelder, R. de, Appelt, S., Wymenga, S.S., Tessari, M., Feiters, M.C., Blumich, B. & Rutjes, F.P.J.T. (2013). Ligand effects of NHC-iridium catalysts for signal amplification by reversible exchange (SABRE). Chemical Communications, 49(67), 7388-7390. http://dx.doi.org/10.1039/c3cc43423k
Willemsen, J.S., Hest, J.C.M. van & Rutjes, F.P.J.T. (2013). Aqueous reductive amination using a dendritic metal catalyst in a dialysis bag. Beilstein Journal of Organic Chemistry, 9, 960-965. http://dx.doi.org/10.3762/bjoc.9.110
Oers, M.C.M. van, Rutjes, F.P.J.T. & Hest, J.C.M. van (2013). Tubular polymersomes: a crosslinker-induced shape transformation. Journal of the American Chemical Society. http://dx.doi.org/10.1021/ja408754z
Delville, M.M.E., Hest, J.C.M. van & Rutjes, F.P.J.T. (2013). Ethyl diazoacetate synthesis in flow. Beilstein Journal of Organic Chemistry, 9, 1813-1818. http://dx.doi.org/10.3762/bjoc.9.211
Delville, M.M.E., Rutjes, F.P.J.T. & Hest, J.C.M. van (2013). Inline work-up in continuous flow chemistry. Abstracts of Papers - American Chemical Society, 245.
Debets, M.F., Hest, J.C.M. van & Rutjes, F.P.J.T. (2013). Bioorthogonal labelling of biomolecules: new functional handles and ligation methods. Organic & Biomolecular Chemistry, 1-17. http://dx.doi.org/10.1039/c3ob41329b
Kalkeren, H.A. van, Delft, F.L. van & Rutjes, F.P.J.T. (2013). Catalytic Appel reactions.Pure and Applied Chemistry, 85(4), 817-828. 10.1351/pac-con-12-06-13
Willemsen, J.S., Hest, J.C.M. van & Rutjes, F.P.J.T. (2013). Potassium formate as a small molecule switch: controlling oxidation-reduction behaviour in a two-step sequence.Chemical Communications, 49(30), 3143-3145. http://dx.doi.org/10.1039/c3cc00126a
Wammes, A.E.M., Fischer, M.J.E., Mol, N.J. de, Eldijk, M.B. van, Rutjes, F.P.J.T., Hest, J.C.M. van & Delft, F.L. van (2013). Site-specific peptide and protein immobilization on surface plasmon resonance chips via strain-promoted cycloaddition. Lab on a Chip, 13(10), 1863-1867. http://dx.doi.org/10.1039/c3lc41338a
Brinkhuis, R.P., Graaf, F. de, Hansen, M.B., Visser, T.R., Rutjes, F.P.J.T. & Hest, J.C.M. van (2013). Dynamically functionalized polymersomes via hydrazone exchange. Polymer Chemistry, 4(5), 1345-1350. 10.1039/c2py20789c
Kalkeren, H.A. van, Blom, A.L., Rutjes, F.P.J.T. & Huijbregts, M.A.J. (2013). On the usefulness of life cycle assessment in early chemical methodology development: the case of organophosphorus-catalyzed Appel and Wittig reactions. Green Chemistry, 15(5), 1255-1263. http://dx.doi.org/10.1039/c3gc00053b
Steendam, R.R.E., Harmsen, B., Meekes, H., Enckevort, W.J.P. van, Kaptein, B., Kellogg, R.M., Raap, J., Rutjes, F. & Vlieg, E. (2013). Controlling the effect of chiral impurities on viedma ripening. Crystal Growth & Design, 13(11), 4776-4780.
Becker, R., Broek, S.A.M.W. van den, Nieuwland, P.J., Koch, K. & Rutjes, F.P.J.T. (2012). Optimisation and Scale-up of alpha-Bromination of Acetophenone in a Continuous Flow Microreactor. Journal of Flow Chemistry, 2(3), 1-5. http://dx.doi.org/10.1556/jfc-d-12-00007
Berkel, S.S. van, Lee, B. van der, Delft, F.L. van, Wagenvoord, R., Hemker, C. & Rutjes, F.P.J.T. (2012). Fluorogenic peptide-based substrates for monitoring thrombin activity.ChemMedChem, 7(4), 606-617. http://dx.doi.org/10.1002/cmdc.201100560
Babich, L., Hartog, A.F., Hemert, L.J. van, Rutjes, Floris & Wever, R. (2012). Synthesis of carbohydrates in a continuous flow reactor by immobilized phosphatase and aldolase.Chemsuschem, 5(12), 2348-53. 10.1002/cssc.201200468
Kalkeren, H.A. van, Rootselaar, S. van, Haasjes, F.S., Rutjes, F.P.J.T. & Delft, F.L. van (2012). Protective group-free synthesis of 3,4-dihydroxytetrahydrofurans from carbohydrates: Formal total synthesis of sphydrofuran. CARBOHYDRATE RESEARCH, 362, 30-37. http://dx.doi.org/10.1016/j.carres.2012.09.004
Becker, R., Broek, S.A.M.W. van den, Nieuwland, P.J., Koch, K. & Rutjes, F.P.J.T. (2012). Optimisation and scale-up of α-bromination of acetophenone in a continuous flow microreactor. Journal of Flow Chemistry, 11(5), 401-407. http://dx.doi.org/10.1556/JFC-D-12-00007
Beer, R.J.A.C. de, Nuijens, T., Wiermans, L., Quaedflieg, P.J.L.M. & Rutjes, F.P.J.T. (2012). Improving the carboxyamidomethyl ester for subtilisin a-catalysed peptide synthesis. Organic & Biomolecular Chemistry, 10(33), 6767-6775. http://dx.doi.org/10.1039/c2ob25662b
Broek, S.A.M.W. van den, Leliveld, J.R., Becker, R., Delville, M.M.E., Nieuwland, P.J., Koch, K. & Rutjes, F.P.J.T. (2012). Continuous flow production of thermally unstable intermediates in a microreactor with inline ir-analysis: Controlled vilsmeier-haack formylation of electron-rich arenes. Organic Process Research & Development, 16(5), 934-938. http://dx.doi.org/10.1021/op2003437
Girones, D., Hanckmann, M., Rutjes, F.P.J.T. & Delft, F.L. van (2012). 2 '-modified neamine analogues from thiomannosides through glycosidation-stereoinversion.European Journal of Organic Chemistry, 2012(31), 4740-4750. http://dx.doi.org/10.1002/ejoc.201200084
Wang, Z.P., Oers, M.C.M. van, Rutjes, F.P.J.T. & Hest, J.C.M. van (2012). Polymersome colloidosomes for enzyme catalysis in a biphasic system. Angewandte Chemie-International Edition, 51(43), 10746-10750. http://dx.doi.org/10.1002/anie.201206555
Georgieva, J.V., Brinkhuis, R.P., Stojanov, K., Weijers, C.A.G.M., Zuilhof, H., Rutjes, F.P.J.T., Hoekstra, D., Hest, J.C.M. van & Zuhorn, I.S. (2012). Peptide-mediated blood-brain barrier transport of polymersomes. Angewandte Chemie-International Edition, 51(33), 8339-8342. http://dx.doi.org/10.1002/anie.201202001
Joosten, L., Laverman, P., Boerman, O.C., Roosenburg, S., Eek, A., Rutjes, Floris & Delft, F.L. van (2012). In vitro and in vivo characterization of three 68Ga- and 111 In-labeled peptides for cholecystokinin receptor imaging. Molecular Imaging, 11(5), 401-407.
Beer, R.J. de, Zarzycka, B., Mariman, M., Amatdjais-Groenen, H., Mulders, M.J., Quaedflieg, P.J.L.M., Delft, F.L. van, Nabuurs, S.B. & Rutjes, F.P.J.T. (2012). Papain-specific activating esters in aqueous dipeptide synthesis. Chembiochem, 13(9), 1319-1326.
Beer, R.J.A.C. de, Bogels, B., Schaftenaar, G., Zarzycka, B., Quaedflieg, P.J.L.M., Delft, F.L. van, Nabuurs, S.B. & Rutjes, F.P.J.T. (2012). Enzyme-Specific Activation versus Leaving Group Ability. Chembiochem, 13(12), 1785-1790.
Brinkhuis, R.P., Stojanov, K., Laverman, P., Eilander, J., Zuhorn, I.S., Rutjes, F.P.J.T. & Hest, J.C.M. van (2012). Size dependent biodistribution and spect imaging of in-111-labeled polymersomes. Bioconjugate Chemistry, 23(5), 958-965. http://dx.doi.org/10.1021/bc200578s
Berkel, S.S. van, Bogels, B.G.M., Wijdeven, M.A., Westermann, B. & Rutjes, F.P.J.T. (2012). Recent advances in asymmetric isocyanide-based multicomponent reactions.European Journal of Organic Chemistry, 2012(19), 3543-3559. http://dx.doi.org/10.1002/ejoc.201200030
Beer, R.J.A.C. de, Zarzycka, B., Mariman, M., Amatdjais-Groenen, H.I.V., Mulders, M.J., Quaedflieg, P.J.L.M., Delft, F.L. van, Nabuurs, S.B. & Rutjes, F.P.J.T. (2012). Papain-specific activating esters in aqueous dipeptide synthesis. Chembiochem, 13(9), 1319-1326. http://dx.doi.org/10.1002/cbic.201200017
Kalkeren, H.A. van, Bruins, J.J., Rutjes, F.P.J.T. & Delft, F.L. van (2012). Organophosphorus-catalysed staudinger reduction. Advanced Synthesis & Catalysis, 354(8), 1417-1421. http://dx.doi.org/10.1002/adsc.201100967
Stojanov, K., Georgieva, J.V., Brinkhuis, R.P., Hest, J.C.M. van, Rutjes, F.P.J.T., Dierckx, R.A.J.O., Vries, E.F.J. de & Zuhorn, I.S. (2012). In vivo biodistribution of prion- and gm1-targeted polymersomes following intravenous administration in mice. Molecular Pharmaceutics, 9(6), 1620-1627. http://dx.doi.org//10.1021/mp200621v
Vervisch, K., D'Hooghe, M., Rutjes, F.P.J.T. & Kimpet, N. De (2012). Chemical and enzymatic synthesis of 2-(2-carbamoylethyl)- and 2-(2-carboxyethyl)aziridines and their conversion into delta-lactams and gamma-lactones. Organic Letters, 14(1), 106-109. http://dx.doi.org/10.1021/ol202888j
Broek, B. van den, Becker, R., Kossl, F., Delville, M.M.E., Nieuwland, P.J., Koch, K. & Rutjes, F.P.J.T. (2012). Prilezhaev dihydroxylation of olefins in a continuous flow process.Chemsuschem, 5(2), 289-292. http://dx.doi.org/10.1002/cssc.201100342
Delville, M.M.E., Gool, J.J.F. van, Wijk, I.M. van, Hest, J.C.M. van & Rutjes, F.P.J.T. (2012). Synthesis of Methoxyisopropyl (MIP)-Protected (R)-Mandelonitrile and Derivatives in a Flow Reactor. Journal of Flow Chemistry, 2(4), 124-128. http://dx.doi.org/10.1556/jfc-d-12-00008
Babich, L., Hemert, J.C. van, Bury, A., Hartog, A.F., Falcicchio, P., Oost, J. van der, Herk, T. van, Wever, R. & Rutjes, F.P.J.T. (2011). Synthesis of non-natural carbohydrates from glycerol and aldehydes in a one-pot four-enzyme cascade reaction. Green Chemistry, 13(10), 2895-2900. hht://dx.doi.org/10.1039/c1gc15429j
Jawalekar, A.M., Reubsaet, E., Rutjes, F.P.J.T. & Delft, F.L. van (2011). Synthesis of isoxazoles by hypervalent iodine-induced cycloaddition of nitrile oxides to alkynes.Chemical Communications, 47(11), 3198-3200. http://dx.doi.org/10.1039/c0cc04646a
Waalboer, D.C.J. & Rutjes, F.P.J.T. (2011). Synthesis and biological activity of novel platencin derivatives. ITB Journal of Science, 43 A(2), 95-112.
Beer, R. de, Zarzycka, B., Amatdjais-Groenen, H.I.V., Jans, S.C.B., Nuijens, T., Quaedflieg, P., Delft, F.L. van, Nabuurs, S.B. & Rutjes, F.P.J.T. (2011). Papain-catalyzed peptide bond formation: Enzyme-specific activation with guanidinophenyl esters. Chembiochem, 12(14), 2201-2207. http://dx.doi.org/10.1002/cbic.201100267
Kalkeren, H.A. van, Leenders, S.H.A.M., Hommersom, C.R.A., Rutjes, F.P.J.T. & Delft, F.L. van (2011). In situ phosphine oxide reduction: A catalytic appel reaction. CHEMISTRY-A EUROPEAN JOURNAL, 17(40), 11290-11295. http://dx.doi.org/10.1002/chem.201101563
Becker, R., Koch, K., Nieuwland, P.J. & Rutjes, F.P.J.T. (2011). Flow chemistry today: Practical approaches for optimisation and scale-up. Chimica Oggi-Chemistry Today, 29(3), 47-49.
Debets, M.F., Van Berkel, S.S., Dommerholt, J., Dirks, A.J., Rutjes, F.P.J.T. & van Delft, F.L. (2011). Bioconjugation with strained alkenes and alkynes. Accounts of Chemical Research, 44(9), 805-815. http://dx.doi.org/10.1021/ar200059z
Malik, H., Kohlen, W., Jamil, M., Rutjes, F.P.J.T. & Zwanenburg, B. (2011). Aromatic a-ring analogues of orobanchol, new germination stimulants for seeds of parasitic weeds.Organic & Biomolecular Chemistry, 9(7), 2286-2293. http://dx.doi.org/10.1039/c0ob00735h
Brinkhuis, R.P., Visser, T.R., Rutjes, F.P.J.T. & van Hest, J.C.M. (2011). Shedding the hydrophilic mantle of polymersomes. Polymer Chemistry, 2(3), 550-552. http://dx.doi.org/10.1039/c0py00316f
Brinkhuis, R.P., Rutjes, F.P.J.T. & Hest, J.C.M. van (2011). Polymeric vesicles in biomedical applications. Polymer Chemistry, 2(7), 1449-1462. http://dx.doi.org/10.1039/c1py00061f
Nieuwland, P.J., Segers, R., Koch, K., van Hest, J.C.M. & Rutjes, F.P.J.T. (2011). Fast scale-up using microreactors: Pyrrole synthesis from micro to production scale. Organic Process Research & Development, 15(4), 783-787. http://dx.doi.org/10.1021/op100338z
Delville, M.M.E., Nieuwland, P.J., Janssen, P., Koch, K., van Hest, J.C.M. & Rutjes, F.P.J.T. (2011). Continuous flow azide formation: Optimization and scale-up. Chemical Engineering Journal, 167(2-3), 556-559. http://dx.doi.org/ 10.1016/j.cej.2010.08.087
Broek, S. van den, Nieuwland, P.J., Koch, K., Laverman, P., Brocken, L., Boerman, O.C. & Rutjes, F.P.J.T. (2011). Fast optimisation of pet tracer synthesis using automated microreactor technology. Journal of Labelled Compounds & Radiopharmaceuticals, 54, S530-S530.
Dommerholt, J., Schmidt, S., Sanders-Temming, R.P., Hendriks, L.J., Rutjes, F.P.J.T., Hest, J.C.M. van, Lefeber, D.J., Friedl, P.H.A. & Delft, F.L. van (2010). Readily accessible bicyclononynes for bioorthogonal labeling and three-dimensional imaging of living cells.Angewandte Chemie-International Edition, 49(49), 9422-5.
Wijdeven, M.A., Willemsen, J.S. & Rutjes, F.P.J.T. (2010). The 3-Hydroxypiperidine Skeleton: Key Element in Natural Product Synthesis. European Journal of Organic Chemistry, 2010(15), 2831-2844.
Wijdeven, M.A., Delft, F.L. van & Rutjes, F.P.J.T. (2010). Synthesis of functionalized 3-hydroxypiperidines. Tetrahedron, 66(30), 5623-5636.
Broek, S.A.M.W. van den, Rensen, P.G.W., Delft, F.L. van & Rutjes, F.P.J.T. (2010). Expedient Pathway into Optically Active 2-Oxopiperidines. European Journal of Organic Chemistry, 2010(30), 5906-5912.
Ritzen, B., Hoekman, S., Verdasco, E.D., Delft, F.L. van & Rutjes, F.P.J.T. (2010). Enantioselective Chemoenzymatic Synthesis of cis- and trans-2,5-Disubstituted Morpholines. Journal of Organic Chemistry, 75(10), 3461-3464.
Malik, H., Rutjes, F.P.J.T. & Zwanenburg, B. (2010). A new efficient synthesis of GR24 and dimethyl A-ring analogues, germinating agents for seeds of the parasitic weeds Striga and Orobanche spp. Tetrahedron, 66(35), 7198-7203.
Malik, H., Rutjes, F.P.J.T. & Zwanenburg, B. (2010). A New Expedient Synthesis of 3-Methyl-2(5H)-furanone, the Common Substructure in Strigolactones, and Its Proposed Biosynthesis. Synthesis-Stuttgart, 2010(19), 3271-3273.
Debets, M.F., Doelen, C.W.J. van der, Rutjes, F.P.J.T. & Delft, F.L. van (2010). Azide: A Unique Dipole for Metal-Free Bioorthogonal Ligations. Chembiochem, 11(9), 1168-1184.
Blanco Ania, D., Valderas-Cortina, C., Hermkens, P.H.H., Sliedregt, L., Scheeren, H.W. & Rutjes, F.P.J.T. (2010). Synthesis of Dihydrouracils Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold. Molecules, 15(4), 2269-2301.
Aslam, W.M., Tabares, L.C., Andreoni, A., Canters, G.W., Rutjes, F.P.J.T. & Delft, F.L. van (2010). 2-Deoxystreptamine conjugates by truncation-derivatization of neomycin.Pharmaceuticals, 3(3), 679-701.
Roosenburg, S., Laverman, P., Joosten, L., Eek, A., Oyen, W.J.G., Jong, M. de, Rutjes, F.P.J.T., Delft, F.L. van & Boerman, O.C. (2010). Stabilized (111)in-labeled sCCK8 analogues for targeting CCK2-receptor positive tumors: synthesis and evaluation.Bioconjugate Chemistry, 21(4), 663-670.
Waalboer, D.C.J., Leenders, S.H., Schulin-Casonato, T., Delft, F.L. van & Rutjes, F.P.J.T. (2010). Total synthesis and antibiotic activity of dehydrohomoplatencin. Chemistry & Biology, 16(37), 11233-6.
Wijk, X.M.R. van, Oosterhof, A., Broek, S.A.M.W. van den, Griffioen, A.W., Dam, G.B. ten, Rutjes, F.P.J.T., Delft, F.L. van & Kuppevelt, A.H.M.S.M. van (2010). A 4-deoxy analogue of N-acetyl-D-glucosamine inhibits heparan sulphate expression and growth factor binding in vitro. Experimental Cell Research, 316(15), 2504-2512.
Nieuwland, P.J., Koch, K., Hest, J.C.M. van & Rutjes, F.P.J.T. (2010). Flow markers in microreactors: a generally applicable chromatographic method for monitoring flow rates during reactions. Open Chemical Engineering Journal, 4, 61-67.
Dommerholt, J., Schmidt, S., Sanders-Temming, R.P., Hendriks, L.J.A., Rutjes, F.P.J.T., Hest, J.C.M. van, Lefeber, D.J., Friedl, P.H.A. & Delft, F.L. van (2010). Readily Accessible Bicyclononynes for Bioorthogonal Labeling and Three-Dimensional Imaging of Living Cells. Angewandte Chemie, International Edition, 49(49), 9422-9425.
Nieuwland, P.J., Koch, K., van Harskamp, N., Wehrens, H.R.M.J., Hest, J.C.M. van & Rutjes, F.P.J.T. (2010). Flash Chemistry Extensively Optimized: High-Temperature Swern-Moffatt Oxidation in an Automated Microreactor Platform. Chemistry-an Asian Journal, 5(4), 799-805.
Debets, M.F., Berkel, S.S. van, Schoffelen, S., Rutjes, F.P.J.T., Hest, J.C.M. van & Delft, F.L. van (2010). Aza-dibenzocyclooctynes for fast and efficient enzyme PEGylation via copper-free (3+2) cycloaddition. Chemical Communications, 46(1), 97-99.
Dirks, A.J., Berkel, S.S. van, Amatdjais-Groenen, H.I.V., Rutjes, F.P.J.T., Cornelissen, J.J.L.M. & Nolte, R.J.M. (2009). Synthesis and aggregation behavior of biohybrid amphiphiles composed of a tripeptidic head group and a polystyrene tail. Soft Matter, 5(8), 1692-1704.
Laverman, P., Meeuwissen, S.A., Berkel, S.S. van, Oyen, W.J.G., Delft, F.L. van, Rutjes, F.P.J.T. & Boerman, O.C. (2009). In-depth evaluation of the cycloaddition--retro-Diels--Alder reaction for in vivo targeting with [(111)In]-DTPA-RGD conjugates. Nuclear Medicine & Biology, 36(7), 749-57.
Koch, K., Berkel, S.S. van, Wal, M. van de, Nieuwland, P.J., Hest, J.C.M. van & Rutjes, F.P.J.T. (2009). Thrombin generation test in microfluidic systems. Journal of Applied Physics, 105(10).
Blanco Ania, D., Hermkens, P.H.H., Sliedregt, L., Scheeren, H.W. & Rutjes, F. (2009). Synthesis of Hydantoins and Thiohydantoins Spiro-Fused to Pyrrolidines: Druglike Molecules Based on the 2-Arylethyl Amine Scaffold. Journal of Combinatorial Chemistry, 11(4), 527-538.
Blanco Ania, D., Hermkens, P.H.H., Sliedregt, L., Scheeren, H.W. & Rutjes, F. (2009). Synthesis of Tetrahydro-beta-carbolines and Tetrahydroisoquinolines Fused to Pyrrolidines and Solution-Phase Parallel Acylation. Journal of Combinatorial Chemistry, 11(4), 539-546.
Blanco Ania, D., Hermkens, P.H.H., Sliedregt, L., Scheeren, H.W. & Rutjes, F. (2009). Solution-Phase Parallel Annulation of (Thio)hydantoins to Tetrahydroisoquinolines and Tetrahydro-beta-carbolines Containing the 2-Arylethyl Amine Scaffold. Journal of Combinatorial Chemistry, 11(4), 547-555.
Blanco Ania, D., Hermkens, P.H.H., Sliedregt, L., Scheeren, H.W. & Rutjes, F. (2009). Synthesis of cucurbitine derivatives: facile straightforward approach to methyl 3-amino-4-aryl-1-methylpyrrolydine-3-carboxylates. Tetrahedron, 65(27), 5393-5401.
Huang, W., Groothuys, S., Heredia, A., Kuijpers, B.H.M., Rutjes, F., Delft, F.L. van & Wang, L.X. (2009). Enzymatic Glycosylation of Triazole-Linked GlcNAc/Glc-Peptides: Synthesis, Stability and Anti-HIV Activity of Triazole-Linked HIV-1 gp41 Glycopeptide C34 Analogues. Chembiochem, 10(7), 1234-1242.
Kaiser, J., Esseveldt, B.C.J. van, Segers, M.J.A., Delft, F.L. van, Smits, J.M.M., Butterworth, S. & Rutjes, F.P.J.T. (2009). Synthesis and aromatisation of cyclic enediyne-containing amino acids. Organic & Biomolecular Chemistry, 7(4), 695-705.
Ritzen, B., Oers, M.C.M. van, Delft, F.L. van & Rutjes, F. (2009). Enantioselective Chemoenzymatic Synthesis of trans-Aziridines. Journal of Organic Chemistry, 74(19), 7548-7551.
Roosenburg, S., Laverman, P., Delft, F.L. van, Eek, A., Rutjes, F. & Boerman, O.C. (2009). Synthesis and characterization of new radiolabeled CCK8 analogues for targeting CCK2 receptor expressing tumors. Amino Acids, 37, 109-109.
Verkade, J.M.M., Pijl, F. van der, Willems, M., Quaedflieg, P., Delft, F.L. van & Rutjes, F. (2009). An Enantioselective Organocatalytic Approach to Both Enantiomers of Lasubine II. Journal of Organic Chemistry, 74(8), 3207-3210.
Waalboer, D.C.J., Kalkeren, H.A. van, Schaapman, M.C., Delft, F.L. van & Rutjes, F.P.J.T. (2009). Total Synthesis and Absolute Stereochemistry of Integric Acid. Journal of Organic Chemistry, 74(22), 8878-8881.
Wijdeven, M.A., Berg, R.J.F. van den, Wijtmans, R., Botman, P.N.M., Blaauw, R.H., Schoemaker, H. E., Delft, F.L. van & Rutjes, F. (2009). Complementary chemoenzymatic routes to both enantiomers of febrifugine. Organic & Biomolecular Chemistry, 7(14), 2976-2980.
Bart, J., Kolkman, A.J., Oosthoek-de Vries, A.J., Koch, K., Nieuwland, P.J., Janssen, J.W.G., Bentum, P.J.M. van, Ampt, K.A.M., Rutjes, F.P.J.T., Wijmenga, S.S., Gardeniers, H. & Kentgens, A.P.M. (2009). A Microfluidic High-Resolution NMR Flow Probe. Journal of the American Chemical Society, 131(14), 5014-5015.
Matteis, V. de, Delft, F.L. van, Tiebes, J. & Rutjes, F. (2008). RCM-mediated synthesis of fluorinated cyclic hydrazines. Synlett, 2008(3), 351-354.
Groothuys, S., Brock, S. van den, Kuijpers, B.H.M., IJsselstijn, M., Delft, F.L. van & Rutjes, F. (2008). Ring-closing alkyne metathesis in the synthesis of alkyne-linked glycoamino acids. Synlett, 2008(1), 111-115.
Hekking, K.F.W., Lefort, L., Vries, A.H.M. de, Delft, F.L. van, Schoemaker, H. E., Vries, J.G. de & Rutjes, F. (2008). Synthesis of versatile building blocks through asymmetric hydrogenation of functionalized itaconic acid mono-esters. Advanced Synthesis & Catalysis, 350(1), 85-94.
Hekking, K.F.W., Waalboer, D.C.J., Moelands, M.A.H., Delft, F.L. van & Rutjes, F. (2008). A ring-closing metathesis approach to cyclic alpha,beta-dehydroamino acids. Advanced Synthesis and Catalysis, 350(1), 95-106.
Jawalekar, A.M., Meeuwenoord, N., Cremers, J.G.O., Overkleeft, H.S., Marel, G.A. van der, Rutjes, F. & Delft, F.L. van (2008). Conjugation of nucleosides and oligonucleotides by [3+2] cycloaddition. Journal of Organic Chemistry, 73(1), 287-290.
Kielbasinski, P., Rachwalski, M.P., Mikolajczyk, M. & Rutjes, F. (2008). Nitrilase-catalysed hydrolysis of cyanomethyl p-tolyl sulfoxide: stereochemistry and mechanism.Tetrahedron-Asymmetry, 19(5), 562-567.
Kuijpers, B.H.M., Groothuys, S., Hawner, C., Dam, J. ten, Quaedflieg, P., Schoemaker, H. E., Delft, F.L. van & Rutjes, F. (2008). Cu-catalyzed formation of triazole-linked glycoamino acids and application in chemoenzymatic peptide synthesis. Organic Process Research & Development, 12(3), 503-511.
Laverman, P., Roosenburg-van Ameijde, S., Gotthardt, M., Park, J.S., Oyen, W.J.G., Jong, M. de, Hellmich, M.R., Rutjes, F., Delft, F.L. van & Boerman, O.C. (2008). Targeting of a CCK2 receptor splice variant with In-111-labelled cholecystokinin-8 (CCK8) and In-111-labelled minigastrin. European Journal of Nuclear Medicine and Molecular Imaging, 35(2), 386-392.
Berkel, S.S. van, Dirks, A.J., Meeuwissen, S.A., Pingen, D.L.L., Boerman, O.C., Laverman, P., Delft, F.L. van, Cornelissen, J.J.L.M. & Rutjes, F. (2008). Application of metal-free triazole formation in the synthesis of cyclic RGD-DTPA conjugates. Chembiochem, 9(11), 1805-1815.
Verkade, J.M.M., Hemert, J.C. van, Quaedflieg, P.J.L.M. & Rutjes, F.P.J.T. (2008). Organocatalysed asymmetric Mannich reactions. Chemical Society Reviews, 37(1), 29-41.
Waalboer, D.C.J., Schaapman, M.C., Delft, F.L. van & Rutjes, F.P.J.T. (2008). High-pressure entry into platencin. Angewandte Chemie-International Edition, 47(35), 6576-6578.
Wijdeven, M.A., Wijtmans, R., Berg, R.J.F. van den, Noorduin, W.L., Schoemaker, H. E., Sonke, T., Delft, F.L. van, Blaauw, R.H., Fitch, R.W., Spande, T.F., Daly, J.W. & Rutjes, F.P.J.T. (2008). N,N-Acetals as N-acyliminium ion precursors: Synthesis and absolute stereochemistry of epiquinamide. Organic Letters, 10(18), 4001-4003.
Koch, K., Rutjes, F.P.J.T. & Hest, J.C.M. van (2008). Bioorganic reactions. In T. Wirth (Ed.),Microreactors in Organic Synthesis and Catalysis (pp. 183-209). [S.l.]: Wiley-VCH.
Laverman, P., Roosenburg-van Ameijde, S., Gotthardt, M., Park, J., Oyen, W.J.G., Jong, M. de, Hellmich, M.R., Rutjes, F.P.J.T., Delft, F.L. van & Boerman, O.C. (2008). Targeting of a CCK(2) receptor splice variant with (111)In-labelled cholecystokinin-8 (CCK8) and (111)In-labelled minigastrin. European Journal of Nuclear Medicine and Molecular Imaging, 35(2), 386-92.
Berkel, S.S. van, Dirks, A.T., Meeuwissen, S.A., Pingen, D.L.L., Boerman, O.C., Laverman, P., Delft, F.L. van, Cornelissen, J.J. & Rutjes, F.P.J.T. (2008). Application of metal-free triazole formation in the synthesis of cyclic RGD-DTPA conjugates. Chembiochem, 9(11), 1805-15.
Aslam, M.W., Busscher, G.F., Weiner, D.P., Gelder, R. de, Rutjes, F. & Delft, F.L. van (2008). Fully orthogonally protected 2-deoxystreptamine from kanamycin. Journal of Organic Chemistry, 73(13), 5131-5134.
Koch, K., Berg, R.J.F. van den, Nieuwland, P.J., Wijtmans, R., Wubbolts, M.G., Schoemaker, H.E., Rutjes, F.P.J.T. & Hest, J.C.M. van (2008). Enzymatic synthesis of optically pure cyanohydrins in microchannels using crude cell lysate. Chemical Engineering Journal, 135, S89-S92.
Koch, K., Berg, R.J.F. van den, Nieuwland, P.J., Wijtmans, R., Schoemaker, H. E., Hest, J.C.M. van & Rutjes, F.P.J.T. (2008). Enzymatic enantioselective C-C-bond formation in microreactors. Biotechnology and Bioengineering, 99(4), 1028-1033.
Kuijpers, B.H.M., Groothuys, S., Soede, A.C., Laverman, P., Boerman, O.C., Delft, F.L. van & Rutjes, F.P.J.T. (2007). Preparation and evaluation of glycosylated arginine-glycine-aspartate (RGD) derivatives for integrin targeting. Bioconjugate Chemistry, 18(6), 1847-54.
Verkade, J.M.M., Hemert, J.C. van, Quaedflieg, P., Schoemaker, H.E., Schurmann, M., Delft, F.L. van & Rutjes, F. (2007). Laccase-mediated deprotection of para-methoxyphenyl (PMP)-protected amines. Advanced Synthesis & Catalysis, 349(8-9), 1332-1336.
Broek, S. van den, Gruijters, B.W.T., Rutjes, F., Delft, F.L. van & Blaauw, R.H. (2007). A short and scalable route to orthogonally O-protected 2-deoxystreptamine. Journal of Organic Chemistry, 72(9), 3577-3580.
Storcken, R.P.M., Panella, L., Delft, F.L. van, Kaptein, B., Broxterman, Q.B., Schoemaker, H.E. & Rutjes, F. (2007). A cross-metathesis route to functionalized alpha-methyl alpha-substituted amino acids. Advanced Synthesis & Catalysis, 349(1-2), 161-164.
Kuijpers, B.H.M., Groothuys, S., Soede, A.C., Laverman, P., Boerman, O.C., Delft, F.L. van & Rutjes, F. (2007). Preparation and evaluation of glycosylated arginine-glycine-aspartate (RGD) derivatives for integrin targeting. Bioconjugate Chemistry, 18(6), 1847-1854.
Kielbasinski, P., Rachwalski, M.P., Wieczorek, W.M., Kwiatkowska, M.S.A., Mikolajczyk, M., Sieron, L. & Rutjes, F. (2007). Enzyme-promoted desymmetrisation of prochiral bis(cyanomethyl)phenylphosphine oxide. Tetrahedron-Asymmetry, 18(17), 2108-2112.
Raijmakers, R., Zendman, A.J.W., Egberts, W.T.M. Vree, Vossenaar, E.R., Raats, J.M.H., Soede-Huijbregts, C., Rutjes, F.P.J.T., Veelen, P.A. van, Drijfhout, J.W. & Pruijn, G.J.M. (2007). Methylation of arginine residues interferes with citrullination by peptidylarginine deiminases in vitro. Journal of Molecular Biology, 367(4), 1118-1129.
Gruijters, B.W.T., Verkade, J.M.M., Delft, F.L. van, Sijbesma, R.P., Hermkens, P.H.H. & Rutjes, F. (2007). A novel purification method in organic synthesis using hydrogen bonding. European Journal of Organic Chemistry, 4197-4204.
Matteis, V. de, Dufay, O., Waalboer, D.C.J., Floris, L.V.D., Tiebes, J. & Rutjes, F. (2007). An improved ring-closing metathesis approach to fluorinated and trifluoromethylated nitrogen heterocycles. European Journal of Organic Chemistry, 2667-2675.
Busscher, G.F., Broek, S. van den, Rutjes, F. & Delft, F.L. van (2007). Carbohydrate mimic of 2-deoxystreptamine for the preparation of conformationally constrained aminoglycosides. Tetrahedron, 63(15), 3183-3188.
Dirks, A.J., Cornelissen, J.J.L.M., Delft, F.L. van, Hest, J.C.M. van, Nolte, R.J.M., Rowan, A.E. & Rutjes, F.P.J.T. (2007). From (bio)molecules to biohybrid materals with the click chemistry approach. QSAR & Combinatorial Science, 26(11-12), 1200-1210.
Berkel, S.S. van, Dirks, A.J., Debets, M.F., Delft, F.L. van, Cornelissen, J.J.L.M., Nolte, R.J.M. & Rutjes, F.P.J.T. (2007). Metal-free triazole formation as a tool for bioconjugation.ChemBioChem., 8, 1504-1508.
Kielbasinski, P., Rachwalski, M.P., Mikolajczyk, M., Szyrej, M., Wieczorek, M.W., Wijtmans, R. & Rutjes, F. (2007). Enzyme-promoted desymmetrisation of prochiral bis(cyanomethyl) sulfoxide. Advanced Synthesis & Catalysis, 349(8-9), 1387-1392.
Matteis, V. de, Delft, F.L. van, Jakobi, H., Lindell, S., Tiebes, J. & Rutjes, F.P.J.T. (2006). RCM-mediated synthesis of trifluoromethyl-containing nitrogen heterocycles. Journal of Organic Chemistry, 71(20), 7527-7532.
Matteis, V. de, Delft, F.L. van, Tiebes, J. & Rutjes, F.P.J.T. (2006). A ring-closing metathesis pathway to fluorovinyl-containing nitrogen heterocyles. European Journal of Organic Chemistry, 1166-1176.
Vink, M.K.S., Wijtmans, R., Reisinger, C., Berg, R.J.F. van den, Schortinghuis, C.A., Schwab, H., Schoemaker, H.E. & Rutjes, F.P.J.T. (2006). Nitrile hydrolysis activity of Rhodococcus erythropolis NCIMB 11540 whole cells. Biotechnology Journal,, 1(5), 569-573.
Verkade, J.M.M., Hemert, J.C. van, Quaedflieg, P., Alsters, P.L., Delft, F.L. van & Rutjes, F.P.J.T. (2006). Mild and efficient deprotection of the amine protecting p-methoxyphenyl (PMP) group. Tetrahedron Letters, 47(46), 8109-8113.
Huibers, M., Manuzi, A., Rutjes, F.P.J.T. & Delft, F.L. van (2006). A sulfitylation-oxidation protocol for the preparation of sulfates. Journal of Organic Chemistry, 71(19), 7473-7476.
Hekking, K.F.W., Moelands, M.A.H., Delft, F.L. van & Rutjes, F.P.J.T. (2006). An in-depth study on ring-closing metathesis of carbohydrate-derived alpha-alkoxyacrylates: Efficient syntheses of DAH, KDO, and 2-deoxy-beta-KDO. Journal of Organic Chemistry, 71(17), 6444-6450.
Groothuys, S., Kuijpers, B.H.M., Quaedflieg, P., Roelen, H., Wiertz, R.W., Blaauw, R.H., Delft, F.L. van & Rutjes, F.P.J.T. (2006). Chemoenzymatic synthesis of triazole-linked glycopeptides. Synthesis-Stuttgart, 3146-3152.
Wijdeven, M.A., Botman, P.N.M., Wijtmans, R., Schoemaker, H.E., Rutjes, F.P.J.T. & Blaauw, R.H. (2005). Total synthesis of (+)-epiquinamide. Organic Letters, 7(18), 4005-4007.
van Lingen, H.L., Delft, F.L. van, Storcken, R.P.M., Hekking, K.F.W., Klaassen, A., Smits, J.M.M., Ruskowska, P., Frelek, J. & Rutjes, F.P.J.T. (2005). Effects of extended aryl-substituted bisoxazoline ligands in asymmetric synthesis - Efficient synthesis and application of 4,4 '-bis(1-naphthyl)-, 4,4 '-bis(2-naphthyl)- and 4,4 '-bis(9-anthryl)-2,2 '-isopropylidenebis(1,3-oxazolines). European Journal of Organic Chemistry, 4975-4987.
Esseveldt, B.C.J. van, Vervoort, P.W.H., Delft, F.L. van & Rutjes, F.P.J.T. (2005). Novel approach to 5-substituted proline derivatives using a silver-catalyzed cyclization as the key step. Journal of Organic Chemistry, 70(5), 1791-1795.
Kaiser, J., Kinderman, S.S., van Esseveldt, B.C.J., Delft, F.L. van, Schoemaker, H.E., Blaauw, R.H. & Rutjes, F.P.J.T. (2005). Synthetic applications of aliphatic unsaturated alpha-H-alpha-amino acids. Organic & Biomolecular Chemistry, 3(19), 3435-3467.
Busscher, G.F., Rutjes, F.P.J.T. & Delft, F.L. van (2005). 2-deoxystreptamine: Central scaffold of aminoglycoside antibiotics. Chemical Reviews, 105(3), 775-791.
Kielbasinski, P., Rachwalski, M.P., Mikolajczyk, M., Moelands, M.A.H., Zwanenburg, B. & Rutjes, F.P.J.T. (2005). Lipase-promoted dynamic kinetic resolution of racemic beta-hydroxyalkyl sulfones. Tetrahedron-Asymmetry, 16(12), 2157-2160.
Kinderman, S.S., Wekking, M.M.T., Maarseveen, J.H. van, Schoemaker, H.E., Hiemstra, H. & Rutjes, F.P.J.T. (2005). Catalytic N-sulfonyliminium ion-mediated cyclizations to a-vinyl-substituted isoquinolines and beta-carbolines and applications in metathesis. Journal of Organic Chemistry, 70(14), 5519-5527.
Kuster, G.J.T., Kalmoua, M., Loevezijn, A. van, Sliedregt, L.A.J.M., Steen, B.J. van, Kruse, C.G., Rutjes, F.P.J.T. & Scheeren, H.W. (2005). Synthesis of spirohydantoins and spiro-2,5-diketopiperazines via resin-bound cyclic alpha,alpha-disubstituted alpha-amino esters. J. Comb.Chem, 8(1), 85-94.
Dirks, A.J.T., Berkel, S.S. van, Hatzakis, N.S., Opsteen, J.A., Delft, F.L. van, Cornelissen, J.J.L.M., Rowan, A.E., Hest, J.C.M. van, Rutjes, F.P.J.T. & Nolte, R.J.M. (2005). Preparation of biohybrid amphiphiles via the copper catalysed Huisgen [3+2] dipolar cycloaddition reaction. Chemical Communications, 4172-4174.
Matteis, V. de, Delft, F.L. van, Gelder, R. de, Tiebes, J. & Rutjes, F.P.J.T. (2004). Fluorinated (hetero)cycles via ring-closing metathesis of fluoride- and trifluoromethyl-functionalized olefins. Tetrahedron Letters, 45(5), 959-963.
Blaauw, R.H., Ijzendoorn, D.R., Cremers, J.G.O., Rutjes, F.P.J.T., Broxterman, Q.B. & Schoemaker, H.E. (2004). Chemo-enzymatic synthesis of chiral fluorine-containing building blocks. Chimia, 58(3), 104-107.
Kinderman, S.S., Gelder, R. de, Maarseveen, M.P. van, Schoemaker, H.E., Hiemstra, H. & Rutjes, F.P.J.T. (2004). Amidopalladation of alkoxyallenes applied in the synthesis of an enantiopure 1-ethylquinolizidine frog alkaloid. Journal of the American Chemical Society, 126(13), 4100-4101.
Wijtmans, R., Vink, M.K.S., Schoemaker, H.E., Delft, F.L. van, Blaauw, R.H. & Rutjes, F.P.J.T. (2004). Biological relevance and synthesis of C-substituted morpholine derivatives. Synthesis-Stuttgart, 641-662.
Busscher, G.F., Rutjes, F.P.J.T. & Delft, F.L. van (2004). Synthesis of a protected enantiomerically pure 2-deoxystreptamine derivative from D-allylglycine. Tetrahedron Letters, 45(18), 3629-3632.
Borsuk, K., Delft, F.L. van, Eggen, I.F., ten Kortenaar, P.B.W., Petersen, A. & Rutjes, F.P.J.T. (2004). Application of substituted 2-(trimethylsilyl)ethyl esters to suppress diketopiperazine formation. Tetrahedron Letters, 45(18), 3585-3588.
IJsselstijn, M., Aguilera, B., Marel, G.A. van der, Boom, J.H. van, Delft, F.L. van, Schoemaker, H.E., Overkleeft, H.S., Rutjes, F.P.J.T. & Overhand, M. (2004). Ring-closing alkyne metathesis mediated synthesis of cyclic beta-turn mimetics. Tetrahedron Letters, 45(22), 4379-4382.
Kinderman, S.S., Maarseveen, J.H. van, Schoemaker, H.E., Hiemstra, H. & Rutjes, F.P.J.T. (2004). C-C bond formation via N-phosphoryliminium ions. Synthesis-Stuttgart, 1413-1418.
Esseveldt, B.C.J. van, Delft, F.L. van, Smits, J.M.M., Gelder, R. de, Schoemaker, H.E. & Rutjes, F.P.J.T. (2004). Transition metal-catalyzed synthesis of novel biologically relevant tryptophan analogues. Advanced Synthesis & Catalysis, 346(7), 823-834.
Kuijpers, B.H.M., Groothuys, S., Keereweer, A.R., Quaedflieg, PJ, Blaauw, R.H., Delft, F.L. van & Rutjes, F.P.J.T. (2004). Expedient synthesis of triazole-linked glycosyl amino acids and peptides. Org Lett, 6(18), 3123-6.
Busscher, G.F., Groothuys, S., Gelder, R. de, Rutjes, F.P.J.T. & Delft, F.L. van (2004). Efficient preparation of a 1,3-diazidocyclitol as a versatile 2-deoxystreptamine precursor.J Org Chem, 69(13), 4477-81.
Botman, PN, Dommerholt, J., Gelder, R. de, Broxterman, Q.B., Schoemaker, H.E., Rutjes, F.P.J.T. & Blaauw, R.H. (2004). Diastereoselective synthesis of (2S,5R)-5-hydroxypipecolic acid and 6-substituted derivatives. Org Lett, 6(26), 4941-4.
Botman, P.N.M., Dommerholt, J., Gelder, R. de, Broxterman, Q.B., Schoemaker, H.E., Rutjes, F.P.J.T. & Blaauw, R.H. (2004). Diastereoselective synthesis of (2S,5R)-5-hydroxypipecolic acid and 6-substituted derivatives. Org Lett, 6, 1523-7060.
Meester, W.J.N., Maarseveen, J.H. van, Kirchsteiger, K., Hermkens, P.H.H., Schoemaker, H.E., Hiemstra, H. & Rutjes, F.P.J.T. (2004). Scope and limitations of the solution and solid phase synthesis of homoallylic amines via N-acyliminium ion reactions. arkivoc, 2, 122-151.
van Esseveldt, B.C.J., Delft, F.L. van, Smits, J.M.M., Gelder, R. de & Rutjes, F.P.J.T. (2003). Pd-catalysed synthesis of 5-substituted proline derivatives from acetylene-containing amino acids. Synlett, 2003(15), 2354-2358.

Further results of scientific activities:

Rutjes, F.P.J.T., Berkel, S.S. van, Dirks, A.J. & Cornelissen, J.J.L.M. (2006) Process for the preparation of 1,4,5-trisubstituted triazoles and 3,4,5-trisubstituted triazoles, 6011073EP.
Verkade, J.M.M., Quaedflieg, P.J.L.M., Alsters, P.L. & Rutjes, F.P.J.T. (2006) Process for the deprotection of protected amines, 6008788EP.
Wiebe, P., Trieu, H., Koch, K., Nieuwland, P.J., Hest, J.C.M. van & Rutjes, F.P.J.T. (2006)Chip holder, fluidic system and chip holder system, PCT/EP2006/010299.
Kuijpers, B.H.M., Groothuys, S., van Delf, t.F.L., Rutjes, F.P.J.T. & Blaauw, R.H. (2005)Preparation of triazole-linked glycoamino acids and glycopeptides.
Drijfhout, J.W., Rutjes, F.P.J.T., Blaauw, R.H., Pruijn, G.J.M., Venrooij, W.J.W. van & Raats, J.M.H. (2004) Peptidylarginine deiminase (PAD) inhibitors, EP 04078481.
Rutjes, F.P.J.T., Storcken, R.P.M., Broxterman, Q.B. & Kaptein, B. (2004) Metathesis reaction involving the unsaturated side chain of an α,α-disubstituted amino acid, WO 2004101476.

Home > Chimica Oggi-Chemistry Today > Vol. 30(2) March/April 2012

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P. 6-8 / FLOW CHEMISTRY
Flow chemistry today: practical approaches for optimisation and scale-up

RENÉ BECKER¹*, KASPAR KOCH¹, PIETER J. NIEUWLAND¹, FLORIS P.J.T. RUTJES²*
*Corresponding authors
1. FutureChemistry Holding B.V., Toernooiveld 100, 6525 EC Nijmegen, The Netherlands
2. Radboud University Nijmegen, Institute for Molecules and Materials, Heyendaalseweg 135, 6525 AJ Nijmegen, The Netherlands

ABSTRACT: A general methodology is presented as a practical approach to the design of a continuous flow process and its subsequent optimisation and up scaling. Three examples of such designs are shown. The continuous flow Swern-Moffatt oxidation shows that even for ultrafast reactions, the same methodology is still feasible, resulting in an 8.5 g/h synthesis rate. Also, the continuous flow synthesis of explosive azides shows that preparative-scale safety issues at a 1 g/h synthesis rate can be more adequately dealt with. Lastly, as an example of what process automation can accomplish, we present the novel application of an automated screening of a model reaction (the Fischer esterification) with on-line gas-chromatographic analysis. Using this set-up, we found optimal reaction conditions within a working day using minimal amounts of reagents and labour, resulting in the continuous production of the target ester at a 67 mL/h rate.

http://teknoscienze.com/articles/chimica-oggi-chemistry-today-flow-chemistry-today-practical-approaches-for-optimisation-and.aspx#.VMD1GEeUc9s

Recent publications:

S. Brauch, Z.P. Wang, M.C.M. van Oers, J.C.M. van Hest, F.P.J.T. Rutjes, "Supramolecular chemical reactors Towards the application of self-assembled polymersomes in cascade reactions", Chim. Oggi. 2014, 32, 73-77.

M.F. Debets, J.S. Prins, D. Merkx, S.S. van Berkel, F.L. van Delft, J.C.M. van Hest, F.P.J.T. Rutjes, "Synthesis of DIBAC analogues with excellent SPAAC rate constants", Org. Biomol. Chem. 2014, 12, 5031-5037. direct link

D.C. Lenstra, F.P.J.T. Rutjes, J. Mecinovic, "Triphenylphosphine-catalysed amide bond formation between carboxylic acids and amines",Chem. Commun. 2014, 50, 5763-5766. direct link

J.S. Willemsen, R.P. Megens, G. Roelfes, J.C.M. van Hest, F.P.J.T. Rutjes, "A One-Pot Oxidation/Enantioselective Oxa-Michael Cascade",Eur. J. Org. Chem. 2014, 2892-2898. direct link

M.C.M. van Oers, L.K.E.A. Abdelmohsen, F.P.J.T. Rutjes, J.C.M. van Hest, "Aqueous asymmetric cyclopropanation reactions in polymersome membranes", Chem. Commun. 2014, 50, 4040-4043. direct link

F. van der Pijl, R.K. Harmel, G.J.J. Richelle, P. Janssen, F.L. van Delft, F.P.J.T. Rutjes, "Organocatalytic Entry into 2,6-Disubstituted Aza-Achmatowicz Piperidinones: Application to (-)-Sedacryptine and Its Epimer", Org. Lett. 2014, 16, 2038-2041. direct link

D. Blanco-Ania, R.W.M. Aben, L.W.A. van Berkom, H.W. Scheeren, F.P.J.T. Rutjes, "High-Pressure-Mediated Extension of the Privileged Steroid Scaffold", Eur. J. Org. Chem. 2014, 1438-1444. direct link

N. Eshuis, N. Hermkens, B.J.A. van Weerdenburg, M.C. Feiters, F.P.J.T. Rutjes, S.S. Wijmenga, M. Tessari, "Toward Nanomolar Detection by NMR Through SABRE Hyperpolarization", J. Am. Chem. Soc. 2014, 136, 2695-2698. direct link

B. Ritzen, G.J.J. Richelle, L. Brocken, F.L. van Delft, F.P.J.T. Rutjes, "Enzyme and Gold Catalysis: A New Enantioselective Entry into Functionalized 4-Hydroxy-2-pyrrolines", Synlett 2014, 25, 270-274. direct link

M. Rachwalski, N. Vermue, F.P.J.T. Rutjes, "Recent advances in enzymatic and chemical deracemisation of racemic compounds", Chem. Soc. Rev. 2013, 42, 9268-9282. direct link

2013

R.P. Brinkhuis, F. de Graaf, M.B. Hansen, T.R. Visser, F.P.J.T. Rutjes, J.C.M. van Hest, "Dynamically functionalized polymersomes via hydrazone exchange", Polym. Chem. 2013, 4, 1345-1350. direct link

H.A. van Kalkeren, F.L. van Delft, F.P.J.T. Rutjes, "Catalytic Appel reactions", Pure Appl. Chem. 2013, 85, 817-828. direct link

H.A. van Kalkeren, A.L. Blom, F.P.J.T. Rutjes, M.A.J. Huijbregts, "On the usefulness of life cycle assessment in early chemical methodology development: the case of organophosphorus-catalyzed Appel and Wittig reactions", Green Chem. 2013, 15, 1255-1263.direct link

A.M. Jawalekar, S. Malik, J.M.M. Verkade, B. Gibson, N. Barta, J.C. Hodges, A. Rowan, F.L. van Delft, "Oligonucleotide tagging for copper-free click conjugation", Molecules 2013, 18, 7346-7363. direct link

P.A.M. Jansen, J.A. van Diepen, B. Ritzen, P.L.J.M. Zeeuwen, I. Cacciatore, C. Cornacchia, I.M.J.J. Vlijmen-Willems, E. de Heuvel, P.N.M. Botman, R.H. Blaauw, P.H.H. Hermkens, F.P.J.T. Rutjes, J. Schalkwijk, "Discovery of Small Molecule Vanin Inhibitors: New Tools To Study Metabolism and Disease", ACS Chem. Biol. 2013, 8, 530-534. direct link

J.S. Willemsen, J.C.M. van Hest, F.P.J.T. Rutjes, "Potassium formate as a small molecule switch: controlling oxidation-reduction behaviour in a two-step sequence", Chem. Commun. 2013, 49, 3143-3145. direct link

R.P. Temming, L. Eggermont, M.B. van Eldijk, J.C.M. van Hest, F.L. van Delft, "N-Terminal Dual Protein Functionalization by Strain-Promoted Alkyne-Nitrone Cycloaddition", Org. Biomol. Chem. 2013, 11, 2772-2779. direct link

J.S. Willemsen, J.C.M. van Hest, F.P.J.T. Rutjes, "Aqueous reductive amination using a dendritic metal catalyst in a dialysis bag",Beilstein J. Org. Chem. 2013, 9, 960-965. direct link

A.E.M. Wammes, M.J.E. Fischer, N.J. de Mol, M.B. van Eldijk, F.P.J.T. Rutjes, J.C.M. van Hest, F.L. van Delft, "Site-specific peptide and protein immobilization on surface plasmon resonance chips via strain-promoted cycloaddition", Lab Chip 2013, 13, 1863-1867. direct link

J.J.F. van Gool, S.A.M.W. van den Broek, R.M. Ripken, P.J. Nieuwland, K. Koch, F.P.J.T. Rutjes, "Highly Controlled Gas/Liquid Processes in a Continuous Lab-Scale Device", Chem. Eng. Technol. 2013, 36, 1042-1046. direct link

J. Garcia-Hartjes, J. Dommerholt, T. Wennekes, F.L. van Delft, H. Zuilhof, "Electronic Effects versus Distortion Energies During Strain-Promoted Alkyne-Azide Cycloadditions: A Theoretical Tool to Predict Reaction Kinetics", Eur. J. Org. Chem. 2013, 3712-3720. direct link

M. Rachwalski, T. Leenders, S. Kaczmarczyk, P. Kielbasinski, S. Lesniak, F.P.J.T. Rutjes, "Efficient catalysts for asymmetric Mannich reactions", Org. Biomol. Chem. 2013, 11, 4207-4213. direct link

B.J.A. van Weerdenburg, S. Gloggler, N. Eshuis, A.H.J. Engwerda, J.M.M. Smits, R. de Gelder, S. Appelt, S.S. Wymenga, M. Tessari, M.C. Feiters, B. Blumich, F.P.J.T. Rutjes, "Ligand effects of NHC-iridium catalysts for signal amplification by reversible exchange (SABRE)",Chem. Commun. 2013, 49, 7388-7390. direct link

T.J. Boltje, T. Heise, F.P.T.J. Rutjes, F.L. van Delft , "A Divergent Method to Prepare 5-Amino-, 5-N-Acetamido-, and 5-N-Glycolylsialosides", Eur. J. Org. Chem. 2013, 5257-5261. direct link

H.A. van Kalkeren, F.L. van Delft, F.P.T.J. Rutjes, "Organophosphorus Catalysis to Bypass Phosphine Oxide Waste", ChemSusChem2013, 6, 1615-1624. direct link

M.M.E. Delville, J.C.M. van Hest, F.P.J.T. Rutjes, "Ethyl diazoacetate synthesis in flow", Beilstein J. Org. Chem. 2013, 9, 1813-1818.direct link

P.A.M. Jansen, P.H.H. Hermkens, P.L.J.M. Zeeuwen, P.N.M. Botman, R.H. Blaauw, P. Burghout, P.M. van Galen, J.W. Mouton, F.P.J.T. Rutjes, J. Schalkwijk, "Combination of Pantothenamides with Vanin Inhibitors as a Novel Antibiotic Strategy against Gram-Positive Bacteria", Antimicrob. Agents Chemother. 2013, 57, 4794-4800. direct link

M.F. Debets, J.C.M. van Hest, F.P.J.T. Rutjes, "Bioorthogonal labelling of biomolecules: new functional handles and ligation methods",Org. Biomol. Chem. 2013, 11, 6439-6455. direct link

R.R.E. Steendam, B. Harmsen, H. Meekes, W.J.P. van Enckevort, B. Kaptein, R.M. Kellogg, J. Raap, F.P.J.T. Rutjes, E. Vlieg, "Controlling the Effect of Chiral Impurities on Viedma Ripening", Cryst. Growth Des. 2013, 13, 4776-4780. direct link

H.A. van Kalkeren, C. te Grotenhuis, F.S. Haasjes, C.A. Hommersom, F.P.J.T. Rutjes, F.L. van Delft, "Catalytic Staudinger/Aza-Wittig Sequence by in situ Phosphane Oxide Reduction", Eur. J. Org. Chem. 2013, 7059-7066. direct link

M.C.M. van Oers, F.P.J.T. Rutjes, J.C.M. van Hest, "Tubular Polymersomes: A Cross-Linker-Induced Shape Transformation", J. Am. Chem. Soc. 2013, 135, 16308-16311. direct link

M. Rachwalski, N. Vermue, F.P.J.T. Rutjes, "Recent advances in enzymatic and chemical deracemisation of racemic compounds", Chem. Soc. Rev. 2013, 42, 9268-9282. direct link

see............
http://www.soc.science.ru.nl/

Synthetic Organic Chemistry
Institute for Molecules and Materials
Radboud University Nijmegen
Heyendaalseweg 135
6525 AJ Nijmegen
The Netherlands

You can contact Prof. Rutjes by email at: F.Rutjes@science.ru.nl

Or by telephone or fax:
Telephone: +31 (0)24 365 3202
Fax: +31 (0)24 365 3393

Secondary functions

Member program committee Fine Chemicals and Pharmaceuticals Cluster CatchBio	(2008 - Heden)
Organic Chemistry training to various companies (occasionally)	(2003 - Heden)
Member program committee STW Perspective Genbiotics	(2010 - Heden)
Co-founder, shareholder and scientific advisor of Chiralix	(2002 - Heden)
Co-founder, shareholder and scientific advisor of FutureChemistry	(2007 - Heden)
Scientific advisor Khondrion	(2010 - Heden)
Member scientific advisory board Leiden‐Amsterdam Centre for Drug Research (LACDR)	(2009 - Heden)
Member Topteam Chemistry and Chairman steering group Innovation Labs	(2010 - Heden)
Co-founder, shareholder and scientific advisor of Pansynt	(2012 - Heden)
Member scientific advisory board J.H. van ‘t Hoff Institute for Molecular Sciences (HIMS/UvA)	(2013 - Heden)
Member Board TKI-NCI	(2014 - Heden)

Lecturer of the following courses:

Organic Chemistry (0), More information
Stereoselective synthesis (1), More information
Industrial Pharmaceutical Chemistry (not in 2014/2015) (2),More information
Application of Metal-catalysis in natural Product Synthesis (not in 2014-2015) (3), More information
Green Chemistry (4), More information
Biocatalysis (not in 2015/2016) (5), More information
Advanced Organic Synthesis (6), More information
Metal Organic Chemistry (7), More information
The future of health: from the laboratory to the clinic and from utopia to applications (8),More information
Synthetic bio-chemistry, nanomedicine and tissue engineering:from research lab to clinic (9), More information