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

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 prod...

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Veröffentlicht in:Journal of organic chemistry 2020-06, Vol.85 (11), p.6844-6853
Hauptverfasser: 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
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container_end_page 6853
container_issue 11
container_start_page 6844
container_title Journal of organic chemistry
container_volume 85
creator 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
description 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.
doi_str_mv 10.1021/acs.joc.0c00473
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