首页> 外国专利> A manufacturing method for optically active 3 - hydroxy pyrrolidine derivatives.

A manufacturing method for optically active 3 - hydroxy pyrrolidine derivatives.

机译:光学活性的3-羟基吡咯烷衍生物的制造方法。

摘要

PURPOSE:To economically and inexpensively obtain the title compound which is an intermediate for medicine by reacting a readily available optically active 4-halo-3-hydroxybutane derivative used as a raw material with a benzylamine derivative. CONSTITUTION:An optically active 4-halo-3-hydroxybutane derivative expressed by formula I (R1 is lower alkyl or phenyl which may have a substituent group; X is halogen; * is asymmetric carbon atom) and used as a raw material is reacted with a benzylamine derivative expressed by formula II (Q is phenyl which may have a substituent group) and preferably used at an amount of equivalent mol to two times by mol, preferably 1.1-1.2 times by mol based on the compound expressed by formula I, in a solvent such as methanol in the presence of an inorganic base such as sodium carbonate to provide the compound expressed by formula III. Furthermore, the compound expressed by formula I is obtained by reacting an optically active 4-halo-1,3-butanediol expressed by formula IV with a sulfonyl compound expressed by formula V.
机译:用途:为了经济而廉价地获得标题化合物,该化合物是医药中间体,通过使容易获得的用作原料的旋光性4-卤代-3-羟基丁烷衍生物与苄胺衍生物反应。组成:一种由式I表示的旋光4-卤代-3-羟基丁烷衍生物(R 1为可具有取代基的低级烷基或苯基; X为卤素; *为不对称碳原子),并用作原料使式II化合物与式II表示的苄胺衍生物(Q为可具有取代基的苯基)反应,相对于式II表示的化合物,其优选使用的摩尔当量为2倍摩尔,优选1.1-1.2倍摩尔Ⅰ,在溶剂如甲醇中,在无机碱如碳酸钠的存在下,得到式Ⅲ表示的化合物。此外,式I表示的化合物是通过使式IV表示的光学活性的4-卤代-1,3-丁二醇与式V表示的磺酰基化合物反应而获得的。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号