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专利概况
专利名称 METHOD FOR PREPARING SUBSTITUTED PHENYLACETIC ACID DERIVATIVE
申请号 WOCN18099121 申请日
公开(公告)号 WO2019047654A1 公开(公告)日 2018-08-07
申请(专利权)人 发明人 LI Jieping; GAO Zhaobo; CHAI Bing; ZHENG Hui; LIU Shengmin; LIU Aqing; GUO Bibao; ZHENG Juncheng; WANG Changfa; LU Weiwei
专利来源 国家知识产权局 转化方式
摘要

The present invention belongs to the field of drug synthesis, and relates to a method for preparing a substituted phenylacetic acid derivative, specifically a method for preparing 2-[4-(2-oxopentylmethyl)phenylpropionic acid]. A precursor compound (I) of loxoprofen is prepared by reacting a dihalobenzyl compound or a disubstituted benzyl compound with a cyclopentanone group or a precursor compound thereof, wherein X is a halogen, L1 is a halogen, OH, OMs, OTs or OTf, L2 is a halogen, a cyano, a hydroxyl, -CH2OH, -CHO, nitromethane, an ester group, -NR4R5, OTf, OTs, OMs, -C=CR6 or -C≡CR7, R4, R5, R6 and R7 are a low substituted alkyl, Z is a cyclopentanone group or a precursor form thereof, the precursor form being (II), (III), (IV), (V) or (VI), and R3 is a low substituted alkyl. Further, the method comprises a step of converting the precursor form of the cyclopentanone group to the cyclopentanone group. The precursor compound of loxoprofen is used for preparing loxoprofen compounds.

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