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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