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PROCESS FOR PRODUCING SUBSTITUTED ALKYLAM INE DERIVATIVE

机译:取代的烷基胺衍生物的制备方法

摘要

The present invention aims at providing a process for producing a substituted alkylamine derivative useful as an intermediate for medicine or agrochemical, from a 2-aminothiophenol derivative at a high yield industrially. The present invention lies in a process for producing a substituted alkylamine derivative represented by the following general formula (3) : CHEM (wherein X is a halogen atom, an alkyl group, an alkoxy group, a cyano group or a nitro group; n is an integer of 1 to 4; and R1 and R2 are each independently a hydrogen atom or a phenyl group-substituted or unsubstituted alkyl group and may together form a 5- or 6-membered ring) or an acid addition salt thereof, which process comprises adding a salt of a 2-aminothiophenol derivative represented by the following general formula (1) : CHEM (wherein X and n have the same definitions as given above) into an acid to allow the system to have a pH of 6 or less and convert the salt into a free 2-aminothiophenol of the general formula (1) and then reacting the 2-aminothiophenol derivative with an amino acid-N-carboxyanhydride represented by the following general formula (2): CHEM (wherein R1 and R2 each have the same definitions as given above).n
机译:本发明的目的是提供一种从2-氨基硫代苯酚衍生物工业上高收率地生产用作医药或农业化学中间体的取代烷基胺衍生物的方法。本发明在于以下通式(3)表示的取代烷基胺衍生物的制造方法:& CHEM&(X为卤原子,烷基,烷氧基,氰基或硝基; n为1至4的整数;并且R 1和R 2各自独立地为氢原子或苯基取代或未取代的烷基,并且可以一起形成5或6元环)或其酸加成盐,该方法包括将由以下通式(1)表示的2-氨基硫代苯酚衍生物的盐添加到酸中,以使体系的pH为6:以下,将其盐转化为通式(1)的游离的2-氨基硫酚,然后使2-氨基硫酚衍生物与下述通式(2)所示的氨基酸-N-羧基酸酐反应: R1和R2的定义与以上n)。

著录项

  • 公开/公告号KR100757641B1

    专利类型

  • 公开/公告日2007-09-10

    原文格式PDF

  • 申请/专利权人

    申请/专利号KR20017015421

  • 发明设计人 히지카타지카라;

    申请日2001-11-30

  • 分类号C07D277/64;

  • 国家 KR

  • 入库时间 2022-08-21 20:31:22

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