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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