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专利概况
专利名称 METHOD FOR REMOVING CARBOXYL AND HYDROXYL PROTECTING GROUP OF β-LACTAM COMPOUND
申请号 WOCN18089760 申请日
公开(公告)号 WO2018233477A1 公开(公告)日 2018-06-04
申请(专利权)人 发明人 CHAI Minjun; YUAN Zhedong; QIAN Jingjie; LI Pengcheng; LUO Jiaying; CHEN Wanglu; CHEN Qingqing; LIU Jing
专利来源 国家知识产权局 转化方式
摘要

The present invention discloses a method for removing a carboxyl and hydroxyl protecting group of a β-lactam compound. The method is removing a carboxyl and/or hydroxyl protecting group from a protected β-lactam compound under the action of trichloroacetic acid and a carbocation absorbent to give a deprotected product of the β-lactam compound. The method of the present invention employs trichloroacetic acid instead of trifluoroacetic acid, and combines trichloroacetic acid with phenol or m-cresol, and anisole, greatly reducing the amount of trichloroacetic acid used. In addition, trichloroacetic acid is decomposed in the presence of water into chloroform and carbon dioxide in a subsequent process converting cephalosporin to a sodium salt, and is easy to remove, without the problem of residual trichloroacetic acid, achieving a high reaction yield and producing relatively few impurities. Trichloroacetic acid is cheap and environmentally friendly and is beneficial in industrial production due to cost reductions achieved.

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