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专利概况
专利名称 METHOD FOR REMOVING CARBOXYL AND HYDROXY PROTECTIVE GROUPS OF LATAMOXEF
申请号 WOCN18089002 申请日
公开(公告)号 WO2018233461A1 公开(公告)日 2018-05-30
申请(专利权)人 发明人 QIAN Jingjie; CHAI Minjun; YUAN Zhedong; 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

Disclosed is a method for removing carboxyl and hydroxy protective groups of latamoxef. The method comprises removing the protective groups of the compound (I) under the action of hydrochloric acid and a carbocation absorbent to obtain the latamoxef acid of the formula (II), wherein R is a hydroxy protective group. The invention uses hydrochloric acid to replace trifluoroacetic acid or aluminum trichloride or tin tetrachloride, and the combination of hydrochloric acid and phenol or m-cresol requires a lower dosage, and is easier to remove, thereby avoiding the problem that trifluoroacetic acid or aluminum and tin ions remain in the final product, resulting in a final product of sub-standard quality; and the residual trace amount of hydrochloric acid forms a trace amount of sodium chloride in the post-treatment salt formation process, wherein same is harmless to the human body. Meanwhile, the method uses hydrochloric acid as an acid catalyst, such that the reaction conditions are mild and the reaction speed is fast, and thus decreasing the cost and the requirement of the production device; and the method has many advantages, such as being efficient, environmentally-friendly, economic, etc., and is suitable for industrial mass production.

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