公开(公告)号：US4898822A

公开(公告)日：1990-02-06

申请号：US846436

申请日：1986-03-31

申请人： Masanori Asada ,  Shigeki Hamaguchi ,  Hidetoshi Katsuki ,  Yoshio Nakamura ,  Hideyuki Takahashi ,  Kenji Takahara ,  Yoshio Shimada ,  Takehisa Ohashi ,  Kiyoshi Watanabe

发明人： Masanori Asada ,  Shigeki Hamaguchi ,  Hidetoshi Katsuki ,  Yoshio Nakamura ,  Hideyuki Takahashi ,  Kenji Takahara ,  Yoshio Shimada ,  Takehisa Ohashi ,  Kiyoshi Watanabe

IPC分类号： C12P17/10 ,  C12P41/00

CPC分类号： C12P17/10 ,  C12P41/005 ,  Y10S435/83 ,  Y10S435/839 ,  Y10S435/843 ,  Y10S435/874 ,  Y10S435/897 ,  Y10S435/911 ,  Y10S435/921 ,  Y10S435/925

摘要： A process for preparing optically active indoline-2-carboxylic acid by an optical resolution, which comprises subjecting a racemic ester of (R,S)-indoline-2-carboxylic acid having the general formula [(R,S)-I] to the action of an enzyme or a microorganism having a stereo-selective esterase activity, which is capable of asymmetrically hydrolyzing the racemic ester [(R,S)-I] to give optically active indoline-2-carboxylic acid having the formula [II*] so as to produce the hydrolysis product, i.e. optically active indoline-2-carboxylic acid [II*] and an unreacted optically active ester of indoline-2-carboxylic acid having the general formula [I*], isolating each optically active form, and further, if necessary, hydrolyzing the obtained optically active ester [I*] to give an optical antipode of the acid [II*].According to the process of the present invention, optically active indoline-2-carboxylic acid with a high optical purity can be prepared in a simple process with a good yield.

摘要翻译： 通过光学拆分制备光学活性二氢吲哚-2-羧酸的方法，其包括使具有通式[（R，S）-I]的（R，S） - 二氢吲哚-2-羧酸的外消旋酯与 具有立体选择性酯酶活性的酶或微生物的作用，其能够不对称地水解外消旋酯[（R，S）-I]，得到具有式[II *]的光学活性二氢吲哚-2-羧酸， ]以产生水解产物，即具有通式[I *]的光学活性二氢吲哚-2-羧酸[II *]和未反应的二氢吲哚-2-羧酸的光学活性酯，分离每种光学活性形式， 此外，如果需要，水解得到的光学活性酯[I *]，得到酸[II *]的光学对映体。 根据本发明的方法，可以以简单的方法制备具有高光学纯度的光学活性二氢吲哚-2-羧酸，产率高。