Publication number: 20210078941
Abstract: The invention belongs to the pharmaceutical manufacturing field, which relates to a novel process for the preparation of substituted phenylacetic acids derivatives, especially relates to the preparation of 2-(4-(2-oxocyclopentyl)phenyl)propanoic acid. The process for the preparation of the precursor form of loxoprofen which use 1,4-di-halobenzyl compounds or disubstituted benzyl compounds as starting material, is through the substitution reaction of cyclopentanone groups or its precursor compounds. Wherein X is halogen, L1 is a suitable leaving group selected from halogen, OH, OMs, OTs, OTf and the like; L2 is a suitable leaving group selected from halogen, CN, OH, —CH2OH, —CHO, CH3NO2, ester group, —NR4R5, OTf, OTs, OMs, —C?CR6, —C?CR7 and the like, wherein R4, R5, R6, R7 are short chain alkyl groups; Z is cyclopentanone group and its precursor form selected from and the like; R3 is short chain alkyl groups.
Type:
Application
Filed:
August 7, 2018
Publication date:
March 18, 2021
Applicant:
Jiangsu Ruike Medical Science And Technology Co., Ltd.
Inventors:
Jieping Li, Zhaobo Gao, Bing Chai, Hui Zheng, Shengmin Liu, Aqing Liu, Bibao Guo, Juncheng Zheng, Changfa Wang, Weiwei Lu