公开(公告)号：EP4357333A1

公开(公告)日：2024-04-24

申请号：EP22824244.2

申请日：2022-06-15

申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

发明人： LI, Xufei ,  WU, Jinlong ,  ZHANG, Yong ,  ZHANG, Yuncai ,  XU, Xiaojie ,  CHEN, Lei ,  WANG, Xiaoming ,  CHEN, Yanan ,  JIN, Meichun ,  ZHOU, Yaqian ,  ZHAN, Dongkai

IPC分类号： C07C303/40

CPC分类号： C07C303/40

摘要： The present invention provides a hybutimibe intermediate and a preparation method therefor. The method comprises the steps of: reacting an easily available raw material of p-fluorobenzoyl butyrate with cheap sulfonylhydrazide to obtain sulfonylhydrazone valerate, then reacting sulfonylhydrazone valerate with carbon dioxide under an alkaline condition to obtain a compound of formula VI with a Z configuration, followed by subjecting the compound of formula VI to acylation, reduction and hydrolysis to obtain the hybutimibe intermediate of (Z)-5-(4-fluorophenyl)-6-hydroxy-hex-4-enoic acid. The preparation method involves readily available and cheap raw materials, has mild reaction conditions, simple and safe operation, a good stereoselectivity, a high yield and low costs, and is suitable for industrial mass production.