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NEW METHOD FOR SYNTHESIZING FEBRIFUGINE AND FEBRIFUGINE COMPOUND

机译:合成新品的新药新品和新品新品

摘要

PROBLEM TO BE SOLVED: To provide a method for synthesizing 2,3-di-substituted piperidines in high stereoselectivity and simply synthesizing febrifugine and its derivative. SOLUTION: A ketone represented by the following chemical formula (1) is reacted with tin (II) triflate and diisopropylethylamine and the reaction product is reacted with 2,3-di-substituted-N-benzyloxycarbonylpiperidine represented by the following chemical formula (2) (R1 and R2 are each a hydrocarbon group which may have same or different substituent group; Cbz is benzyloxycarbonyl group) in the presence of Lewis acid and the reaction product is treated with a strong acid to produce the objective febrifugine represented by the following chemical formula (3).
机译:解决的问题:提供一种高立体选择性地合成2,3-二取代的哌啶并简单地合成非来福定及其衍生物的方法。解决方案:由以下化学式(1)表示的酮与三氟甲磺酸锡(II)和二异丙基乙胺反应,反应产物与由以下化学式(2)表示的2,3-二取代-N-苄氧基羰基哌啶反应(R 1和R 2各自为可具有相同或不同取代基的烃基; Cbz为苄氧羰基),并且在路易斯酸存在下,将反应产物用强酸处理,以产生由以下化学式表示的目标非铁夫定(3)。

著录项

  • 公开/公告号JP2002201192A

    专利类型

  • 公开/公告日2002-07-16

    原文格式PDF

  • 申请/专利权人 JAPAN SCIENCE & TECHNOLOGY CORP;

    申请/专利号JP20000403394

  • 发明设计人 KOBAYASHI OSAMU;

    申请日2000-12-28

  • 分类号C07D401/06;A61K31/517;A61P33/06;C07D211/40;

  • 国家 JP

  • 入库时间 2022-08-22 00:58:43

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