Reflections on Chirality in the Pharmaceutical Industry: Past, Present and Future Dr. Christopher J. Welch, Distinguished Scientist Process Research & Development Merck Research Laboratories, USA

Christopher Welch

New Technologies, Postdoc Program, Science Lead, Analytical Chemistry at Merck

christopher_welch@merck.com

Reflections on Chirality in the Pharmaceutical Industry: Past, Present and Future Dr. Christopher J. Welch, Distinguished Scientist Process Research & Development Merck Research Laboratories, USA   





A PRESENTATION

   

At Chiral India 2016, New horizons in Drug development, Harnessing the power of Chirality .Organised by chemical weekly at Holiday inn international, Mumbai, India, Nov 8 2016

Christopher J. Welch

Science Lead for Analytical Chemistry
Merck Research Laboratories

Christopher J. Welch is Science Lead for Analytical Chemistry within the Process and Analytical Chemistry area at Merck Research Laboratories in Rahway, NJ.  Chris leads the New Technologies Review and Licensing Committee (NT-RLC), the organization that oversees identification, acquisition and evaluation of new technologies of potential value to Merck Research Laboratories.  Chris also leads the MRL Postdoctoral Research Fellows Program.  He received his BS degrees in Chemistry and Biochemistry from the University of Illinois at Urbana-Champaign in 1982 and a Ph.D. degree in Organic Chemistry (also U of I) in 1992. Dr. Welch has worked in a variety of fields within the chemical industry, including discovery synthesis of agrochemicals (Velsicol-Sandoz), development of reagents for improved immunodiagnostic assays (Abbott Laboratories), and development and commercialization of chromatographic stationary phases, reagents and enantioselective catalysts within a small chemical business environment (Regis Technologies).  Since joining Merck in 1999, he has focused on developing and applying improved methods and equipment for purification, synthesis and analysis of pharmaceuticals and intermediates.  Dr. Welch has authored more than 230 scientific publications and patents.  He is co-founder of the journal, Enantiomer, a current or past member of the editorial advisory boards for the journals, Chirality, Organic & Biomolecular Chemistry, Journal of the Korean Chemical Society, Chemistry World, Chemical & Engineering News and ACS Central Science.  Chris is past chair of the ACS Division of Organic Chemistry (ORGN), a member of the Executive Committee for the International Symposia on Chirality, a member of the ACS steering committee for Pacifichem and a member of the PittCon Program Resource Team.  Honors and awards include the NJCG Award for Excellence in Chromatography (2004), the PACS Activated Carbon Hall of Fame award (2007), MRL Presidents Award for Environmental Achievement (2009), Microsoft Life Science Innovation Award (2010), Fellow of the American Chemical Society (2010), Fellow of the American Association for the Advancement of Science, AAAS (2013), the Chirality Medal (2015) and the University of Nebraska Industrial Advisory Board Award (2016).

Experience

Distinguished Scientist, Process & Analytical Chemistry

Merck & Co., Inc.

May 1999 – Present (17 years 8 months)Rahway, NJ

Current responsibilities: Scientific Lead, Analytical Chemistry co-chair, New Technologies Review & Licensing Committee (NT-RLC) co-chair, Merck Research Laboratories Postdoctoral Research Fellows Committee

Previous Positions at Merck: Science Lead, Global Analytical Chemistry 8/10 – 8/12 Distinguished Senior Investigator, Process Research 7/07 – 8/10 Associate Director. Process Research 1/06 – 6/07 Senior Research Fellow, Process Research 6/03 – 12/05 Research Fellow, Process Research 5/99 – 6/03

Director of Research

Regis Technologies

May 1992 – March 1999 (6 years 11 months)Morton Grove, IL (Chicago area)

- New product development and commercialization (chromatography columns, reagents, enantioselective catalysts) - Scientific evaluation of custom organic synthesis business - Set up contract synthesis/preparative chromatographic separation business - first of kind

Honors & Awards

Fellow

American Association for the Advancement of Science (AAAS)

October 2012

Fellow

American Chemical Society (ACS)

August 2010

Chirality Medal 2015

January 2015

Presidential Green Chemistry Award

US Environmental Protection Agency

June 2014

– for precompetitive collaboration between Merck, Pfizer, Eli Lilly and University of Wisconsin on Aerobic Oxidation Methods for Pharmaceutical Synthesis - co-awardees: Shannon Stahl and Thatcher Root (U. Wisconsin), Joel Hawkins (Pfizer) and Joe Martinelli (Lilly)

Industrial Advisory Board (IAB) Award

University of Nebraska Department of Chemistry

March 2016

Inaugural IAB award from U. Nebraska recognizing excellence in scientific research in an industry setting

Organizations

American Chemical Society, Division of Organic Chemistry (ORGN)

Councilor and Chair

January 2006 – December 2015

Pacifichem

Member of Steering Committee for Pacifichem 2020

Starting August 2011

Chirality (Journal)

member, editorial board

Starting March 2002

Chemical & Engineering News

member, editorial advisory board

Starting February 2012

Chemistry Today (RSC)

member, editorial advisory board

Starting March 2011

Journal of the Korean Chemical Society

member, international advisory board

Starting February 2011

Pittcon

Member, Pittcon Program Committee Resource Team

Starting May 2012

ACS Central Science

Member of Editorial Advisory Board

Starting January 2015

American Chemical Society

Member, Committee on Science (ComSci

Starting January 2016

Publications

2014 publications, part 1

Use of a Miniature Mass Spectrometer to Support Pharmaceutical Process Research Investigations, Org. Proc. R&D 18, 103-108, 2014.

Chromatographic Separation and Assignment of Absolute Configuration of Hydroxywarfarin Isomers, Chirality 26, 95-101, 2014. Chromatographic Resolution of Closely Related Species in Pharmaceutical Chemistry: Dehalogenation Impurities and Mixtures of Halogen...more

2014 publications - part 2

Precompetitive Collaboration on Enabling Technologies for the Pharmaceutical Industry, Org. Proc. R&D 18, 481–487, 2014.

Imine-based Chiroptical Sensing Approach for Analysis of Chiral Amines: From Method Design to Synthetic Application, Chem. Sci. 5, 2855-2861, 2014. Advances in Achiral Stationary Phases for SFC, Amer. Pharm. Rev., April 2014, 36-41. Liquid Chromatography Methods for...more

2013 Publications

Evaluation of core–shell particle columns for ion-pair reversed-phase liquid chromatography analysis of oligonucleotides, J. Pharm. Biomed. Anal. 72, 25–32, 2013.

Pharmaceutical Industry Practices on Genotoxic Impurities, in Pharmaceutical Industry Practices on Genotoxic Impurities, ed Heewoon Lee, Taylor & Francis, 2013. Rapid Analysis of Residual Palladium in Pharmaceutical...more

2012 Publications
2012

A Simple Parallel Gas Chromatography Column Screening System, Wes Schafer, Simon E. Hamilton, Zainab Pirzada and Christopher J. Welch, Chirality, 24,1–4, 2012.

Rapid catalyst identification for the synthesis of the pyrimidinone core of HIV integrase inhibitors, A. Bellomo, N. Celebi-Olcum, X. Bu, N. Rivera, R.T. Ruck, C.J. Welch, K.N. Houk, S.D. Dreher, Angew. Chem. Int. Ed., 51 (2012) 1-5 ...more

2011 Publications

Application of Ion Mobility Spectrometry in Drug Substance Development, H. Gao, X. Jia, R. Xiang, X. Gong, C. Welch, Analytical Methods, 3, 1828-1837, 2011.

Analytical Method Volume Intensity Index:A Green Chemistry Metric for HPLC Methodology in the Pharmaceutical Industry, R. Hartman, R. Helmy, M. Al-Sayah, C. Welch, Green Chemistry 13, 934-939, 2011. Does an Axial Propeller Shape on a...more

2010 Publications

High-throughput metal screening in pharmaceutical samples by ICP-MS with automated flow injection using a modified HPLC configuration, Tu, Wang, Welch, J. Pharm. Biomed. Anal., 51, 90-95, 2010.

Systematic Evaluation of New Chiral Stationary Phases for Supercritical Fluid Chromatography Using a Standard Racemate Library, Pirzada, Personick, Biba, Gong, Zhou, Schafer, Welch, J. Chromaogr.A,...more

Adsorbent Screening for Metal Impurity Removal in Pharmaceutical Process(Link)

Organic Process Research & Development

February 23, 2005

A microtube screening approach affords simple and convenient assessment of the selective adsorption of metal impurities by a variety of different process adsorbents. This approach is helpful in identifying rapid solutions to metal impurity problems in pharmaceutical process research. Several examples illustrating the utility of the approach are presented.

Online Analysis of Flowing Streams Using Microflow HPLC

Organic Process Research & Development

2009

Supercritical fluid chromatography for GMP analysis in support of pharmaceutical development and manufacturing activities(Link)

Journal of Pharmaceutical and Biomedical An

Response to Comment on “Cocktail Chromatography: Enabling the Migration of HPLC to Nonlaboratory Environments”(Link)

ACS Sustainable Chem. Eng. 2015, 3 (9), 1897.

ACS Sustainable Chem. Eng. 2015, 3 (9), 1897.

Education

University of Illinois at Urbana-Champaign

Ph.D., Organic Chemistry

1996 – 1999

The University of Chicago

FUELING INNOVATION

Welch helped launch Merck's new postdoctoral research fellowship program.

/////////Reflections on Chirality in the Pharmaceutical Industry, Past, Present and Future Dr. Christopher J. Welch, Distinguished Scientist, Process Research & Development,  Merck Research Laboratories, USA, presentation

Dr.B Gopalan CSO & Executive Director, Drug Discovery Research, Orchid Chemicals and Pharmaceuticals Limited,

Gopalan B

Chief Scientific Officer,Drug Discovery Research, at Orchid Research Laboratories Limited,

 

 LINK

 http://182.73.176.174/chc/scientists/Dr_Gopalan.pdf

 https://in.linkedin.com/in/gopalan-b-b78b627


Dr.Balasubramanian Gopalan CSO & Executive Director, Drug Discovery Research, Orchid Chemicals and Pharmaceuticals Limited, Sholinganallur, Chennai.

Email: drbgopalan@yahoo.co.in

Dr.Balasubramanian Gopalan a Ph.D. in the year 1973 from University of Madras in Synthetic Organic Chemistry and worked as Post Doctoral fellow in Harvard University with Nobel laurite E.J.Corey and then switched over to the industry and joined Syntex Research Inc., California and Bristol-Myers Squibb in Newjersey, USA.

He returned to India in the year 1982 and headed drug discovery division of Boots Pharmaceuticals Ltd., Sun Pharma Advanced Research Centre, Glaxo Ltd., Glenmark Research Centre, Matrix Laboratories and finally join as Executive Director and Chief of Orchid Chemicals & Pharmaceuticals in the year 2008.

His achievements include discoveries of many new drugs that are in Phase-2 and Phase-3 clinical trial. Many of these discoveries such as Oglemilast (a novel PDE IV inhibitor) was out-licensed to Forest Laboratories, USA for US$190 million over a period of five years & also to Teijin of Japan for US$53 million.

Other of his drug melogliptin a new DPP4 for type 2 diabetes was out-licensed to Merck Germany for US$231 million.

He has been a visiting fellow and elected fellow of many academics and universities to his credit he has 50 international patents.

He shares his expertise by training local talents in drug discovery research from Orchid chemical & Pharmaceuticals Ltd., OMR, Chennai.

Experience

Chief Scientific Officer,Drug Discovery Research,

Orchid Research Laboratories Limited,

CSO

Orchid Chemicals and Pharmaceuticals Ltd

2008 – Present (8 years)

Education

University of Madras

1970 – 1976

ICOS21, IIT BOMBAY, DEC 2016

DR B GOPALAN, CSO & Executive Director,
Drug Discovery Research, Orchid Chemicals and
Pharmaceuticals Limited,Sholinganallur,Chennai. — with DR B GOPALAN, ORCHID.

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Dr Joelle Prunet

• Senior Lecturer (Chemistry)

telephone: 01413308774
email: Joelle.Prunet@glasgow.ac.uk

A4-13 Organic Section, Chemistry, Joseph Black Building, Glasgow G12 8QQ




links
https://uk.linkedin.com/in/joelle-prunet-36954315

Experience

Senior Lecturer - Head of Organic Chemistry

University of Glasgow

August 2009 – Present (7 years 5 months)

Directrice de Recherche

CNRS

October 2003 – August 2009 (5 years 11 months)

Education

Harvard University

PhD, Organic Chemistry

1987 – 1993

PhD advisor: Professor David A. Evans

Ecole Normale Superieure Paris

BsC

1984 – 1987

Lycee Saint-Genevieve

1981 – 1984

Research Interests

The main research interest of the Prunet group is the synthesis of biologically active natural products, such as taxol, a powerful antitumor agent, or dolabelide C and hexacyclinic acid, molecules with cytotoxic activity. In our approaches towards the target molecules, we uncover problems that cannot be easily solved by known reactions, and to overcome these difficulties we try to develop new methodologies that can also be applied to other syntheses.

‌‌  Publication Highlights

• Gamba-Canchez, D.; Prunet, J. J. Org. Chem. 2010, 75, 3129-3132 Synthesis of Modified Methyl Furanosides by Intramolecular Oxa-Michael Reaction followed by Pummerer Rearrangement.
• Ma, C.; Schiltz, S.; Le Goff, Xavier F.; Prunet, J. Chem. Eur. J. 2008, 7314-7323 Ring-Closing Metathesis in the Synthesis of BC Ring-Systems of Taxol.
• Toueg, J.; Prunet J. Org. Lett. 2008, 10, 45-48 Dramatic Solvent Effect on the Diastereoselectivity of Michael Addition: Study towards the Synthesis of the ABC Ring-System of Hexacyclinic Acid.
• Rotulo-Sims, D.; Prunet J. Org. Lett. 2007, 9, 4147-4150 Tandem Conjugate Addition-Elimination for the Diastereoselective Synthesis of 4E-Alkenyl Syn 1,3-Diols.
• Vincent, A.; Prunet, J. Synlett 2006, 2269-2271 Enantioselective Synthesis of the C1-C15 Fragment of Dolabelide C.

Ma, C., Letort, A., Aouzal, R., Wilkes, A., Maiti, G., Farrugia, L. J., Ricard, L., and Prunet, J. (2016) Cascade metathesis reactions for the synthesis of taxane and isotaxane derivatives. Chemistry: A European Journal, 22(20), pp. 6891-6899. (doi:10.1002/chem.201600592) (PMID:27062670)

Letort, A., Aouzal, R., Ma, C., Long, D.-L., and Prunet, J. (2014) Highly efficient synthesis of the tricyclic core of Taxol by cascade metathesis.Organic Letters, 16(12), pp. 3300-3303. (doi:10.1021/ol501304j)

Chevalley, A., Prunet, J., Mauduit, M., and Ferezou, J.-P. (2013) Model studies for a ring-closing metathesis approach to the Bafilomycin macrolactone core from a 2,2-dimethoxy tetraenic ester precursor.European Journal of Organic Chemistry, 2013(36), pp. 8265-8278.(doi:10.1002/ejoc.201300559)

Redon, S., Wierzbicki,, M., and Prunet, J. (2013) A new oxa-michael reaction and a gold-catalysed cyclisation en route to C-glycosides.Tetrahedron Letters, 54(16), pp. 2089-2092.(doi:10.1016/j.tetlet.2013.02.022)

Prunet, J. (2011) Progress in metathesis through natural product synthesis. European Journal of Organic Chemistry, 2011(20-21), pp. 3634-3647. (doi:10.1002/ejoc.201100442)

Braun, M.G., Vincent, A., Boumediene, M., and Prunet, J. (2011) Highly demanding cross metathesis in the synthesis of the C16-C30 fragment of dolabelide C. Journal of Organic Chemistry, 76(12), pp. 4921-4929.(doi:10.1021/jo200466t)

Gamba-Sanchez, D., and Prunet, J. (2010) Synthesis of modified methyl furanosides by intramolecular oxa-Michael reaction followed by Pummerer rearrangement. Journal of Organic Chemistry, 75(9), pp. 3129-3132. (doi:10.1021/jo100241e)

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