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US 10,479,753 B2Granted
Sacubitril intermediate and preparation method thereof
AssigneeSunshine Lake Pharma Co., Ltd.
InventorsLei Chen, Guodong Sun, Xiaodong Han, Shun Li, Jiebin Zeng, Zhongqing Wang, Zhonghua Luo
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Abstract
The present invention relates to a sacubitril intermediate and a preparation method thereof. The sacubitril intermediate disclosed herein can be prepared by a deprotection reaction of a compound. In addition, the intermediate can be used as a raw material to synthesize sacubitril. The method disclosed herein has advantages of easily obtained raw materials, simple preparation process, low cost, environment friendly, and etc., which is very suitable for industrial production.
Claims16
A method of preparing sacubitril,
- comprising the following steps:
- a) preparing a compound of Formula (VI) by an enzymic catalytic reaction of a compound of Formula (V) in the presence of ω-transaminase and phosphopyridoxal,
- b) optionally, preparing a compound of Formula (VII) from the compound of Formula (VI):
- c) preparing sacubitril from the compound of Formula (VII),
- wherein:
- R1 is phenyl, methoxy, hydroxy, chloro, bromo, iodo, mesylate, triflate or 4-methylbenzenesulfonate;
- R2 is
- R3 is H, —(C1-C4)alkyl or —(C1-C4)alkyl-aryl;
- and
- R4 is H, —(C1-C4)alkyl, —(C3-C6)heterocyclyl, —(C1-C4)alkyl-aryl, trimethylsilyl, triethylsilyl or t-butyldimethylsilyl.
7 more elements
Dependencies are inferred from the claim text.