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Application of Transition-Metal Catalysis, Biocatalysis and Flow Chemistry as State-of-the-Art Technologies in the Synthesis of LCZ696

Gu, Wayne and Zhao, Jibin and Li, Yunzhong and Yu, Bo and Tian, Xiangguang and Min, Jacob and Xu, Su and Gu, Huijuan and Sun, Junjie and Wang, Xufan and Ye, Shengqing and Yang, Hongwei and Tian, Yingtao and Gao, Feng and Gai, Yu and Wang, Yan and Zhang, Xuesong and Luo, Xi and Schenkel, Berthold and Venturoni, Francesco and Filipponi, Paolo and Guelat, Bertrand and Allmendinger, Thomas and Hoehn, Pascale and Kovacic, Nikola and Hermann, Luca and Schlama, Thierry and Ruch, Thomas and Derrien, Nadine and Piechon, Philippe and Kleinbeck-Riniker, Florian and Chen, Like and Wang, Huaimin and Wietfeld, Bernhard and Zhao, Stephen and Chang, Tommy and Lu, Xiaoquan and Zhang, Jianghua and Wu, Jingjing and Jia, Guanghua and Liu, Weichun and Gu, Xin and Hai, Dong (2020) Application of Transition-Metal Catalysis, Biocatalysis and Flow Chemistry as State-of-the-Art Technologies in the Synthesis of LCZ696. The Journal of Organic Chemistry. ISSN 0022-32631520-6904

Abstract

LCZ696 is a novel treatment for patients suffering from heart failure that combines the two active pharmaceutical ingredients sacubitril and valsartan in a single chemical compound. While valsartan is an established drug substance, a new manufacturing process suitable for large-scale commercial production had to be developed for sacubitril. The use of chemocatalysis, biocatalysis, and flow chemistry as state-of-the-art technologies allowed to efficiently build up the structure of sacubitril and achieve the defined performance targets.

Item Type: Article
Date Deposited: 02 Jun 2020 00:45
Last Modified: 02 Jun 2020 00:45
URI: https://oak.novartis.com/id/eprint/40789

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