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

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

View Resource (DOI)

Category

Peer-reviewed journal

Published on CMKC

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.

Journal

Journal of Organic Chemistry. Volume 85, 2020, 6844–6853

DOI

10.1021/acs.joc.0c00473

Type of publication

Peer-reviewed journal

Affiliations

  • Suzhou Novartis Technical Development Co., Ltd.
  • Novartis Pharmaceuticals (China) Suzhou Operations
  • Novartis Pharma AG

Article Classification

Research Article

Classification Areas

  • Intermediate

Tags

  1. biocatalysis
  2. chemocatalysis
  3. heart failure
  4. Intermediate
  5. LCZ696
  6. Research Article