公开(公告)号：EP1026163B1

公开(公告)日：2006-03-22

申请号：EP98944223.1

申请日：1998-09-24

申请人： IHARA CHEMICAL INDUSTRY CO., LTD.

发明人： UMEZU, Kazuto, Ihara Chemical Industry Co., Ltd ,  TANIGUCHI, Shuji, Ihara Chemical Industry Co., Ltd ,  OGAWA, Mahito, Ihara Chemical Industry Co., Ltd ,  HIYOSHI, Hidetaka, Ihara Chem. Industry Co., Ltd

IPC分类号： C07D277/64

CPC分类号： C07D277/64

摘要： A process for producing substituted alkylamines of general formula (3) or salts thereof, characterized by reacting a metal salt of a 2-aminothiophenol derivative of general formula (1) with an amino acid N-carboxy anhydride of general formula (2) and cyclizing the obtained product under acidic conditions. By this process, substituted alkylamines typified by 1-(2-benzothiazolyl)alkylamines and salts thereof can be produced in high yields from 2-aminothiophenol derivatives on an industrial scale while keeping excellent handling properties. Even when the intended substituted alkylamine is an optically active compound, the intended product can be produced without reducing the optical purity of the optically active starting material.

公开(公告)号：EP1026163A1

公开(公告)日：2000-08-09

申请号：EP98944223.1

申请日：1998-09-24

申请人： IHARA CHEMICAL INDUSTRY CO., LTD.

发明人： UMEZU, Kazuto, Ihara Chemical Industry Co., Ltd ,  TANIGUCHI, Shuji, Ihara Chemical Industry Co., Ltd ,  OGAWA, Mahito, Ihara Chemical Industry Co., Ltd ,  HIYOSHI, Hidetaka, Ihara Chem. Industry Co., Ltd

IPC分类号： C07D277/64

CPC分类号： C07D277/64

摘要： The present invention provides a process for producing a substituted alkylamine represented by the following general formula (3):
or a salt thereof, which process comprises reacting a 2-aminothiophenol derivative metal salt represented by the following general formula (1):
with an amino acid-N-carboxy anhydride represented by the following general formula (2):
and then subjecting the reaction product to cyclization under an acidic condition.
According to the present invention, a substituted alkylamine typified by 1-(2-benzthiazolyl)alkylamine, or a salt thereof can be produced from a 2-aminothiophenol derivative industrially at a high handleability at a high yield; even when the intended substituted alkylamine is an optically active compound, the intended product can be produced without reducing the optical purity of optically active raw material.

摘要翻译： 本发明提供由以下通式（3）表示的取代烷基胺的制备方法：其中CHEM或其盐包括使下述通式（1）表示的2-氨基苯硫酚衍生金属盐与下述通式 ＆lt; CHEM＆gt;与下述通式（2）表示的氨基酸-N-羧酸酐：，然后使反应产物在酸性条件下环化。 根据本发明，以2-（2-苯并噻唑基）烷基胺为代表的取代烷基胺或其盐可以以高收率工业上高处理性的2-氨基苯硫酚衍生物制备; 即使目标取代的烷基胺是光学活性化合物，也可以在不降低光学活性原料的光学纯度的情况下制造目的产物。