Gu, Wayne, Zhao, Jibin, Li, Yunzhong, Yu, Bo, Tian, Xiangguang, Min, Jacob, Xu, Su, Gu, Huijuan, Sun, Junjie, Wang, Xufan, Ye, Shengqing, Yang, Hongwei, Tian, Yingtao, Gao, Feng, Gai, Yu, Wang, Yan, Zhang, Xuesong, Luo, Xi, Schenkel, Berthold, Venturoni, Francesco, Filipponi, Paolo, Guelat, Bertrand, Allmendinger, Thomas, Hoehn, Pascale, Kovacic, Nikola, Hermann, Luca, Schlama, Thierry, Ruch, Thomas, Derrien, Nadine, Piechon, Philippe, Kleinbeck-Riniker, Florian, Chen, Like, Wang, Huaimin, Wietfeld, Bernhard, Zhao, Stephen, Chang, Tommy, Lu, Xiaoquan, Zhang, Jianghua, Wu, Jingjing, Jia, Guanghua, Liu, Weichun, 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