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US 11,370,739 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.
Claims16
A compound of Formula (V),
- wherein:
- R1 is phenyl, methoxy, hydroxy, chloro, bromo, iodo, mesylate, triflate or 4-methylbenzenesulfonate;
- R2 is
- with the proviso that when R1 is phenyl, R2 is not
- 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.
4 more elements
A method of preparing a compound of Formula (V):
- wherein the compound of Formula (V) is prepared by a deprotection reaction of a compound of Formula (IV):
- in the presence of a base or an acid, wherein:
- R1 is phenyl, methoxy, hydroxy, chloro, bromo, iodo, mesylate, triflate or 4-methylbenzenesulfonate;
- R2 is
- with the proviso that when R1 is phenyl, R2 is not
- R3 is H, —(C1-C4)alkyl or —(C1-C4)alkyl-aryl;
- R4 is H, —(C1-C4)alkyl, —(C3-C6)heterocyclyl, —(C1-C4)alkyl-aryl, trimethylsilyl, triethylsilyl or t-butyldimethylsilyl;
- and
- R5 is H, —(C1-C4)alkyl or —(C1-C4)alkyl-aryl.
6 more elements
Dependencies are inferred from the claim text.