首页> 外国专利> PROCESS FOR PRODUCING O-ALKYLATED RAPAMYCIN DERIVATIVE, AND O-ALKYLATED RAPAMYCIN DERIVATIVE

PROCESS FOR PRODUCING O-ALKYLATED RAPAMYCIN DERIVATIVE, AND O-ALKYLATED RAPAMYCIN DERIVATIVE

机译:O-烷基化雷帕霉素衍生物和O-烷基化雷帕霉素衍生物的生产方法

摘要

A process for producing an O-alkylated rapamycin derivative of high purity, i.e. a purity is not lower than 99%, is porivided. A process for producing an o-alkylated rapamycin derivative represented by the following general formula (1) is provided. The process includes the steps of reacting rapamycin with an alkyl triflate, purifying a reaction product, which has been obtained by the above reaction, with a normal phase chromatograph and further purifying a purified product, which has been purified with the normal phase chromatograph, with a reverse phase chromatograph wherein R represents alkyl, arylalkyl, hydroxyalkyl, alkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl, alkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.
机译:制备高纯度,即纯度不低于99%的O-烷基化雷帕霉素衍生物的方法。提供一种由以下通式(1)表示的邻烷基化雷帕霉素衍生物的制备方法。该方法包括以下步骤:使雷帕霉素与三氟甲磺酸烷基酯反应,用正相色谱仪纯化通过上述反应获得的反应产物,并进一步纯化用正相色谱仪纯化的纯化产物。反相色谱仪其中R代表烷基,芳基烷基,羟烷基,烷氧基烷基,酰氧基烷基,氨基烷基,烷基氨基烷基,烷氧基羰基氨基烷基,酰基氨基烷基或芳基。

著录项

  • 公开/公告号EP2090580B1

    专利类型

  • 公开/公告日2014-06-04

    原文格式PDF

  • 申请/专利权人 TERUMO KABUSHIKI KAISHA;

    申请/专利号EP20070831792

  • 发明设计人 KAWANISHI TETSURO;ISOZAKI MASASHI;

    申请日2007-11-14

  • 分类号C07D498/18;B01D9/02;B01D15/08;

  • 国家 EP

  • 入库时间 2022-08-21 15:51:07

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