Practical Synthesis of 5,7-Dichlorotetrahydroisoquinoline-6-carboxylic Acid─Key Intermediate of Lifitegrast (Xiidra)

Author:

Liu Xu1,Guo Heng1,Peng Peng2,Li Yaping3,Yang Jiangtao1,Wu Chuanjun1,Xu Shengjun4,Zhao Chuanmeng1ORCID,Zhang Fuli1

Affiliation:

1. Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Pudong District Shanghai 201203, China

2. Collaborative Innovation Center of Yangtze River Delta Region Green Pharmaceuticals, Zhejiang University of Technology, Hangzhou 310014, China

3. School of Chemistry and Chemical Engineering, Shanghai University of Engineering and Science, Songjiang District Shanghai 201620, China

4. Zhejiang Boxiao Biopharmaceutical Co. Ltd, Hangzhou 310014, China

Funder

Zhejiang Boxiao Biopharmaceutical Co., Ltd

China State Institute of Pharmaceutical Industry

Publisher

American Chemical Society (ACS)

Subject

General Chemical Engineering,General Chemistry

Reference16 articles.

1. Lifitegrast: A novel drug for treatment of dry eye disease

2. Discovery and Development of Potent LFA-1/ICAM-1 Antagonist SAR 1118 as an Ophthalmic Solution for Treating Dry Eye

3. Burnier, J.; Gadek, T.; Naud, F. Crystalline pharmaceutical and methods of preparation and use thereof. WO2009139817A2, 2009.

4. Burnier, J.; Gadek, T.; Naud, F. LFA-1 inhibitor and polymorph thereof. WO2014018748A1, 2014.

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