81025-83-4Relevant articles and documents
Application of Transition-Metal Catalysis, Biocatalysis, and Flow Chemistry as State-of-the-Art Technologies in the Synthesis of LCZ696
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
, p. 6844 - 6853 (2020/06/04)
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.
CYCLIC PHOSPHATE SUBSTITUTED NUCLEOSIDE DERIVATIVES FOR THE TREATMENT OF LIVER DISEASES
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Page/Page column 66; 67, (2018/06/06)
The present invention relates to Compounds of Formula (I) or Formula (II) or a pharmaceutically acceptable salt, solvate or enantiomer thereof, wherein A, B, R1, R2, R3, R4, Q and V are as defined herein. The present invention also relates to pharmaceutical compositions comprising a Compound of Formula (I) or Formula (II) and to their use in therapy.
Spirobenzylamine-Phosphine, Preparation Method Therefor And Use Thereof
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Paragraph 0080; 0081, (2014/07/22)
The present invention relates to a spirobenzylamine-phosphine, preparation method therefor and use thereof. The compound has a structure represented by formula (I), wherein n=0 to 3; R1, R2, R3, R4, R5, R6, R7, R8 and R9 having a value as defined in claim 1. Starting from the substituted 7-trifluoromesyloxy-7′-diarylphosphino-1,1′-spiro-dihydroindene, the compound is synthesized in a two-step or three-step reactions. The new spirobenzylamine-phosphine is complexed with an iridium precursor and is subjected to ion exchange, to give an Iridium/spirobenzylamine-phosphine complex comprising various anions. The spiro benzyl amine-phosphine/Iridium complex according to the present invention may be used for catalyzing asymmetry hydrogenation of a variety of alpha-substituted acrylic acids, has high activity and enantio-selectivity, and has a good prospect of industrialization.