Zai-Xin Chen, Director of R&D Center at Jiangsu Yabang Pharmaceutical Group Co., Ltd

Zai-Xin Chen

Director of R&D Center at Jiangsu Yabang Pharmaceutical Group Co., Ltd

LINKS

https://cn.linkedin.com/in/zai-xin-chen-45074179

https://www.researchgate.net/profile/Zai_Xin_Chen

zaixin_chen@163.com

Experience

Director of R&D Center

Jiangsu Yabang Pharmaceutical Group Co., Ltd

Visiting Scientist

National Research Council Canada

2002 – 2003 (1 year)

Postdoctoral Researcher

RWTH Aachen University

August 2000 – February 2002 (1 year 7 months)Aachen, Germany

Education

Chengdu University of Science and Technology

Jiangsu Yabang Pharmaceutical Group Co., Ltd

Yabang Chemical Group Co., Ltd is one of key 100 cultivation enterprises of JiangSu Province, high-tech enterprises in Jiangsu Province, the State Torch Program key high-tech enterprises, with a post-doctoral research station and provincial level technical center, ranked as one of the top 50 in China's petrochemical industry. "YABANG "trademark is approved by the State Administration for Industry and Commerce Trademark Office as" China's well-known trademarks. " Yabang Chemical Group Co., Ltd. always adheres to the business philosophy as "people-oriented, technology-first, quality and the credit as the most important things", adheres to the strategic objectives as "to fight for the No.1 in the industry in China, and to fight for the No.1 in the products in the world" and to develop well and fast! Yabang chemicals group is approved by the National Administration for Industry and Commerce as a private enterprises group with the Yabang Chemical Group Co., Ltd. as the core , which is trans-regional and cross-sectoral, integrating science, industry, and trade as a whole. Now under the Group, there are four major industries as dyes, paints, pharmaceutical, real estate. The Group has More than 7,000 employees, covers an area of 2.8 million square meters, with total assets of 3 billion yuan. In 2006, the sales amounted to 6 billion yuan, creating profits and taxes 450 million yuan.

REGIOMER OF BESIFLOXACIN





Abstract: In this paper (R)-7-(azepan-3-ylamino)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride 1 was isolated and identified as the N-substituted regioisomer of besifloxacin, which has been synthesized from the reaction of 8-chloro-1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 3 with (R)-tert-butyl 3-aminoazepane-1-carboxylate 2 in acetonitrile as solvent in 37% yield. The chemical structure of compound 1 was established on the basis of 1H-NMR, 13C-NMR, mass spectrometry data and elemental analysis.
Structural Characterization
1H-NMR (500 MHz, DMSO-d6): δ ppm: 14.73 (H-23, s, 1H), 9.72 (H-14, s, 2H), 8.69 (H-7, s, 1H),7.79 (H-1, d, J = 13.1 Hz, 1H), 6.20 (H-11, d, J = 9.1 Hz, 1H), 4.37 (H-12 and H-19, m, 2H), 3.38(H-13, m, 2H), 3.23 (H-15, m, 1H), 3.09 (H-15, m, 1H), 2.14 (H-18, m, 1H), 1.94 (H-16 and H-18, m,2H), 1.84 (H-16 and H-17, m, 2H), 1.60 (H-17, m, 1H), 1.23 (H-20 or H-21, m, 2H), 1.03 (H-20 orH-21, m, 2H).
13C-NMR(125 MHz, DMSO-d6): δ ppm: 175.6 (C-9), 165.4 (C-22), 151.7 (C-7), 150.6 (C-2), 148.7(C-3), 139.0 (C-5), 137.3 (C-4), 117.8 (C-10), 110.3 (C-1), 107.0 (C-8), 52.9 (C-12), 50.1 (C-13), 46.2(C-15), 41.3 (C-19), 34.0 (C-18), 24.9 (C-16), 21.6 (C-17), 10.9 (C-20 or C-21).
FAB-MS, m/z = 394.1 (M+).
Elemental analysis: Calculated for C19H21ClFN3O3.HCl: C, 53.03%; H, 5.15%; N, 9.77%; found: C,52.82%; H, 5.39%; N, 9.50%.

1H-NMR (500 MHz, DMSO-d6): δ ppm: 14.73 (H-23, s, 1H), 9.72 (H-14, s, 2H), 8.69 (H-7, s, 1H), 7.79 (H-1, d, J = 13.1 Hz, 1H), 6.20 (H-11, d, J = 9.1 Hz, 1H), 4.37 (H-12 and H-19, m, 2H), 3.38 (H-13, m, 2H), 3.23 (H-15, m, 1H), 3.09 (H-15, m, 1H), 2.14 (H-18, m, 1H), 1.94 (H-16 and H-18, m,2H), 1.84 (H-16 and H-17, m, 2H), 1.60 (H-17, m, 1H), 1.23 (H-20 or H-21, m, 2H), 1.03 (H-20 orH-21, m, 2H).

 

13C-NMR(125 MHz, DMSO-d6): δ ppm: 175.6 (C-9), 165.4 (C-22), 151.7 (C-7), 150.6 (C-2), 148.7(C-3), 139.0 (C-5), 137.3 (C-4), 117.8 (C-10), 110.3 (C-1), 107.0 (C-8), 52.9 (C-12), 50.1 (C-13), 46.2(C-15), 41.3 (C-19), 34.0 (C-18), 24.9 (C-16), 21.6 (C-17), 10.9 (C-20 or C-21).

PAPER

Molbank 2013, 2013(2), M801; doi:10.3390/M801

Short Note

(R)-7-(Azepan-3-ylamino)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic Acid Hydrochloride

Zhengjun Xia, Zaixin Chen *  and Shuitao Yu

 http://www.mdpi.com/1422-8599/2013/2/M801

Supplementary File 3:Support Information (PDF, 340 KB)

Download PDF [188 KB, 27 May 2013; original version 22 May 2013]

R&D Center, Jiangsu Yabang Pharmaceutical Group, Changzhou 213200, China

In this paper (R)-7-(azepan-3-ylamino)-8-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid hydrochloride 1was isolated and identified as the N-substituted regioisomer of besifloxacin, which has been synthesized from the reaction of 8-chloro-1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid 3 with (R)-tert-butyl 3-aminoazepane-1-carboxylate 2in acetonitrile as solvent in 37% yield. The chemical structure of compound 1 was established on the basis of ¹H-NMR, ¹³C-NMR, mass spectrometry data and elemental analysis

REGIOMER OF BESIFLOXACIN

BESIFLOXACIN

 

 Zaixin Chen *
R&D Center, Jiangsu Yabang Pharmaceutical Group, Changzhou 213200, China
* Author to whom correspondence should be addressed;

E-Mail: zaixin_chen@163.com.

CHANGZHOU

///////////

Zhiyong Wang

Zhiyong Wang

WANG Zhiyong（汪志勇）

Ph.D., University of Science and Technology of China (USTC) (1992); M.S., USTC (1989); B.S., Anhui Normal University (1982).


Professor of Chemistry
Department of Chemistry
School of Chemistry and Materials Science
University of Science and Technology of China
Hefei, Anhui 230026, P. R. China
Tel: 86-551-63603185
Fax: 86-551-63603185
E-mail: zwang3@ustc.edu.cn
Personal Homepage:
http://staff.ustc.edu.cn/~zwang3/default.htm

RESEARCH INTERESTS
Research in our group will focus on the general areas of reaction development and chemical synthesis. Our studies will be driven by the discovery of new and useful catalysts. By virtue of the developed organic reactions various organic ligands are synthesized and used as probes in biological progress. Brief summaries of three research directions illustrating these objectives are shown below:
1) The preparation of heterogeneous catalysts;
2) The theoretical calculation for the mechanism of organic reactions;
The application of organic ligands as probes or inhibitors to explore the molecular mechanism of HIV transcription.
PUBLICATIONS
http://www.researcherid.com/rid/F-7955-2010

WANG Zhiyong, Professor

Name: Zhiyong Wang（汪志勇） Born: June, 1962, Anhui, P. R. China Address: Department of Chemistry, University of Science and Technology of China, 230026 Hefei, P. R. China Tel: 86-551-63603185 Fax: 86-551-63603185 E-mail: zwang3@ustc.edu.cn EDUCATION AND RESEARCH EXPERIENCE 　1978-1982 B.S., Anhui Normal University 　1982-1986 Lecturer, South Anhui Agricultural College, China 　1986-1989 M.S., University of Science and Technology of China 　1989-1992 Ph.D., University of Science and Technology of China 　1992-1997 Lecturer, Associate Professor, University of Science and Technology of China 　1997-1999 Research Fellow, Tulane University & Brandeis University 　1999-Now Professor of Chemistry, University of Science and Technology of China RESEARCH INTERESTS 1) Organic reactions in aqueous media and development of synthetic methodology; 2) Supramolecular assembly under the control of organic ligands; 3) Drug design on the base of PCAF bromodomain. CURRENT RESEARCH PROJECTS 1) Organic reactions in water mediated by nano-metals and its application in asymmetric synthesis, National Natural Science Foundation (2004-2006) 2) Crystal Engineering under control of organic ligands, Foundation from Education Department of Anhui Province (2003-2005) REPRESENTATIVE PUBLICATIONS 1) C-F. Pan, M. Meze, S. Mujtaba, M. Muller, L. Zeng, J-M. Li, Z-Y. Wang,* M-M. Zhou* “Structure-Guided Optimization of Small Molecules Selectively Inhibiting HIV-1 Tat and PCAF Association” J. Med. Chem., 2007, 50, 2285 2) Y. Xie, Z-P. Yu, X-Y. Huang, Z-Y. Wang,* L-W. Niu, M-K. Teng, J. Li “Rational Design on the MOFs Constructed from modified Aromatic Amino Acids” Chem. Eur. J., 2007, 13, 9399 3) Z-H. Zhang, C-F. Pan, Z-Y. Wang* “Synthesis of chromanones: a novel palladium-catalyzed Wacker-type oxidative cyclization involving 1,5-hydride alkyl to palladium migration” Chem. Commun, 2007, 4686 4) Y. Xie, Y. Yan, H-H. Wu, G-P. Yong, Y. Cui, Z-Y. Wang*, L. Pan, J. Li “Homochiral Metal-organic Coordination Networks from L-Tryptophan” Inorg. Chim. Acta., 2007, 360,1669 5) Y. Xie, H-H. Wu, G-P. Yong,, Z-Y. Wang*, R. Fan , R-P. Li, G-Q. Pan, Y-C. Tian, L-S. Sheng, L. Pan, J. Li “Synthesis, Crystal Structure, Spectroscopic and Magnetic Properties of Two Cobalt Molecules Constructed from Histidine” J. Mol. Struct., 2007, 833, 88 6) Z-H. Zhang, Z-Y. Wang* “Diatomite-Supported Pd Nanoparticles: An Efficient Catalyst for Heck and Suzuki Reactions” J. Org. Chem., 2006, 71, 7485 7) Z-H. Zhang, Z-G. Zha, C-S. Gan, C-F. Pan, Y-Q. Zhou, Z-Y. Wang*, M-M. Zhou* “Catalysis and Regioselectivity of the Aqueous Heck Reaction by Pd(0) Nanoparticles under Ultrasonic Irradiation” J. Org. Chem., 2006, 71, 4339

Scheme 1
Control experiments.
The ubiquitous oxazoles have attracted more and more attention in both industrial and academic fields for decades. This interest arises from the fact that a variety of natural and synthetic compounds which contain the oxazole substructure exhibit significant biological activities and antiviral properties. Although various synthetic methodologies for synthesis of oxazols have been reported, the development of milder and more general procedure to access oxazoles is still desirable.

Initially, compound A, formed by the substitution reaction of 1a with 2a, which can be transformed following two pathways: (a) I⁺, generated by the oxidation of iodine, could oxidize A to radical intermediate B, which eliminates one molecular of CO₂ to generate radical C, which is further oxidized to imine Dor its isomer E. Subsequently, F is obtained by intramolecular nucleophilic addition of E. Finally, the desired product (3a) is given by deprotonation and oxidation of F; (b) G is formed from the oxidation of A. Then 3a is obtained through H, I, J, K following a process similar to path a.

Scheme 2
Plausible mechanism.

General procedure for the synthesis of polysubstituted oxazoles

1a (105.8 mg, 0.7 mmol), 2a (99.5 mg, 0.5 mmol), I₂ (50.8 mg, 0.2 mmol), DMA (2 mL) and TBHP (70% aqueous solution, 1 mmol) were placed in a tube (10 mL) and sealed with a thin film. Then the reaction mixture was stirred at 25°C for 4 h, heated up to 60°C and stirred at this temperature for another 4 h. After that, the resulting mixture was cooled to the room temperature, diluted with water, extracted with ethyl acetate. The organic phase was washed with saturation sodium chloride solution, dried and filtrated. The solvent was evaporated under reduced pressure and the residue was purified by silica gel column separation (petroleum ether:ethyl acetate = 10:1) to give 3a(154.7 mg, 70%) as light yellow solid, mp = 70–72°C.
2,5-diphenyloxazole (3a) [1]
Synthesized according to typical procedure and purified by column chromatography (petroleum ether:ethyl acetate = 10:1) to give light yellow solid (154.7 mg, 70%), mp = 70-72 °C.

1H NMR (300 MHz, CDCl3): δ 8.12-8.09 (m, 2 H), 7.72-7.69 (m, 2 H), 7.50-7.40 (m, 6 H), 7.35-7.24 (m, 1 H).

13C NMR (75 MHz, CDCl3): δ 161.3, 151.4, 130.4, 129.0, 128.9, 128.5, 128.1, 127.6, 126.4, 124.3, 123.6.

HRMS (APCI-FTMS) m/z: [M + H]+ calcd for C15H12NO: 222.0913, Found: 222.0911.

The scope of the reaction. Standard conditions: 0.7 mmol of amino acids (1a-1h), 0.5 mmol of2a-2j, 0.1 mmol of I₂, 1 mmol of TBHP, 2 mL of DMA, were stirred at 25°C for 4 h then slowly raised to 60°C for 4 h. Catalysts amount and isolated yields were based on 2.

Metal-free synthesis of polysubstituted oxazoles via a decarboxylative cyclization from primary α-amino acids

Yunfeng Li, Fengfeng Guo, Zhenggen Zha and Zhiyong Wang^*

• *Corresponding author: Zhiyong Wang zwang3@ustc.edu.cn

Zhiyong Wang

Department of Chemistry, Hefei National Laboratory for Physical Sciences at Microscale, CAS Key Laboratory of Soft Matter Chemistry, University of Science and Technology of China, Hefei, Anhui 230026, P. R. China

Sustainable Chemical Processes 2013, 1:8  doi:10.1186/2043-7129-1-8
The electronic version of this article is the complete one and can be found online at:http://www.sustainablechemicalprocesses.com/content/1/1/8

ADDITIONAL SPECTRAL DATA FROM NET

Hefei, Anhui China






 

 




////Metal-free,  Synthesis,  Oxazoles,  Oxidation,  Decarboxylative cyclization,  α-amino acids

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WUXI JINXIN BIOSCIENCES CO., LTDwas founded in 2013 It is an integrated chemistry CRO and CMO and focuses on developing pharmaceutical intermediates, peptide, cosmetic ingredients and dietary supplement ingredients, from lab scale to full scale manufacturing. After years of operation, our technological management team consists of experienced Ph.D. and M.S. who are familiar with the industry. Located in Wuxi New District, 2 hour driving from Shanghai, China, JINXIN BIOSCIENCES is dedicated to provide the global biotechnology and pharmaceutical industries with professional chemistry services. We owns 53, 820 sft total standing alone R& D building in Wuxi with 13 synthetic labs, 1 kilo lab and 1 analytical lab. Our R& D building is equipped with Bruker 400MH NMR, Agilent 1200 HPLC, Analytical LCMS, Preparative LCMS, GCMS, Microwave synthesizers and other modern equipments. We have two cooperative plants with reactors from 50L to 5000L, low temperature vessels ( -80¡ æ ) and high pressure and temperature vessels ( 12MPa, 250¡ æ ) . Our compounds can be scaled up to tons in our manufacturing base with some other equipments, such as rectification column, muti-function workshop, clean workshop and so on. We put top priority on the belief of super quality, punctual delivery, reasonable prices, best reputation and would like to have cooperate and create value with all customer for together. Jiangsu China /common/images/branded/RA/images/30936_g5.jpgAriel View at the Ramada Parkview Hotel in Changzhou Jiangsu, ChinaChangzhou Jiangsu, China Tongli village, Jiangsu, China.jpg