- 专利标题: HYBUTIMIBE INTERMEDIATE AND PREPARATION METHOD THEREFOR
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申请号: EP22824244.2申请日: 2022-06-15
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公开(公告)号: EP4357333A1公开(公告)日: 2024-04-24
- 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
- 申请人: Zhejiang Hisun Pharmaceutical Co., Ltd.
- 申请人地址: CN Taizhou, Zhejiang 318000 No.46 Waisha Road Jiaojiang District
- 专利权人: Zhejiang Hisun Pharmaceutical Co., Ltd.
- 当前专利权人: Zhejiang Hisun Pharmaceutical Co., Ltd.
- 当前专利权人地址: CN Taizhou, Zhejiang 318000 No.46 Waisha Road Jiaojiang District
- 代理机构: Dehns
- 优先权: CN 202110669168 2021.06.17
- 国际申请: CN2022098917 2022.06.15
- 国际公布: WO2022262768 2022.12.22
- 主分类号: C07C303/40
- IPC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.
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