公开(公告)号：US08993800B2

公开(公告)日：2015-03-31

申请号：US13897079

申请日：2013-05-17

申请人： Kaneka Corporation

发明人： Takahiro Ohishi ,  Hirokazu Nanba ,  Masanobu Sugawara ,  Masashi Izumida ,  Tatsuya Honda ,  Kohei Mori ,  Satohiro Yanagisawa ,  Nobuo Nagashima ,  Kenji Inoue

IPC分类号： C07C315/00 ,  C12P13/12 ,  C07C319/06 ,  C07D233/76 ,  C12P17/04 ,  C12P17/10 ,  C12P41/00

CPC分类号： C12P13/12 ,  C07C319/06 ,  C07D233/76 ,  C12P17/04 ,  C12P17/10 ,  C12P41/009 ,  C07C323/58

摘要： The present invention provides a simple industrial process for producing an L- or D-optically active α-methylcysteine derivative or its salt, which is a useful pharmaceutical intermediate, from readily available, inexpensive raw materials. In a process for producing an L- or D-optically active α-methylcysteine derivative or its salt, a racemic N-carbamoyl-α-methylcysteine derivative or its salt is D-selectively cyclized with hydantoinase to produce a D-5-methyl-5-thiomethylhydantoin derivative or its salt and an N-carbamoyl-α-methyl-L-cysteine derivative or its salt, which are then subjected to deprotection of the amino group and the sulfur atom, and hydrolysis.

摘要翻译： 本发明提供了一种简单的工业方法，用于从容易获得的便宜的原料制备作为有用的药物中间体的L-或D-光学活性的α-甲基半胱氨酸衍生物或其盐。 在制备L-或D-光学活性α-甲基半胱氨酸衍生物或其盐的方法中，外消旋的N-氨基甲酰基-α-甲基半胱氨酸衍生物或其盐与乙内酰脲酶D选择性环化以产生D-5-甲基 - 5-硫代甲基乙内酰脲衍生物或其盐和N-氨基甲酰基-α-甲基-L-半胱氨酸衍生物或其盐，然后进行氨基和硫原子的脱保护和水解。