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    • 2. 发明授权
    • Method for optical resolution of DL-cysteine and (R,S)-1-(1-naphthyl)
ethylamine
    • DL-半胱氨酸和(R,S)-1-(1-萘基)乙胺的光​​学拆分方法
    • US4736060A
    • 1988-04-05
    • US892059
    • 1986-08-01
    • Keizo TomuroYoshiharu TamuraYoko MorimotoShigeyoshi Katoh
    • Keizo TomuroYoshiharu TamuraYoko MorimotoShigeyoshi Katoh
    • C07D277/06C07B57/00
    • C07D277/06
    • Method for optical resolution of DL-cysteine by (1) reacting DL-cysteine with formaldehyde to prepare DL-thiazolidine-4-carboxylic acid (DL-TCA), (2) forming diastereomer salts of D-TCA and of L-TCA by reacting DL-TCA with an optically active 1-(1-naphthyl)ethylamine, (3) separating said diastereomer salts by difference of the solubilities thereof in a solvent, (4) recovering D-TCA from said diastereomer salt of D-TCA and finally obtain D-cysteine, and recovering L-TCA from said diastereomer salt of L-TCA and finally obtain L-cysteine.Method for optical resolution of (R,S)-1-(1-naphthyl)ethylamine (R,S)-NEA by (1) reacting an optically active cysteine with formaldehyde to prepare an optically active thiazolidine-4-carboxylic acid, (2) forming diastereomer salts of (R)-NEA and of (S)-NEA by reacting (R,S)-NEA with optically active thiazolidine-4-carboxylic acid, (3) separating said diastereomer salts of (R)-NEA and of (S)-NEA by difference of the solubilities thereof in a solvent, (4) recovering (R)-NEA from said diastereomer salt of (R)-NEA, and recovering (S)-NEA from said diastereomer salt of (S)-NEA.
    • (1)使DL-半胱氨酸与甲醛反应以制备DL-噻唑烷-4-羧酸(DL-TCA),(2)形成D-TCA和L-TCA的非对映异构体盐的方法,通过 使DL-TCA与光学活性1-(1-萘基)乙胺反应,(3)通过溶剂中溶解度的差异分离所述非对映异构体盐,(4)从D-TCA的非对映体盐中回收D-TCA和 最后得到D-半胱氨酸,从L-TCA的非对映异构体盐中回收L-TCA,最后得到L-半胱氨酸。 (1)将光学活性半胱氨酸与甲醛反应制备光学活性噻唑烷-4-羧酸的(R,S)-1-(1-萘基)乙胺(R,S)-NEA的光学拆分方法, 2)通过使(R,S)-NEA与光学活性噻唑烷-4-羧酸反应形成(R)-NEA和(S)-NEA的非对映异构体盐,(3)将(R)-NEA的所述非对映异构体盐 和(S)-NEA的溶解度的差异,(4)从(R)-NEA的所述非对映体盐中回收(R)-NEA,并从(R)-NEA的所述非对映异构体盐中回收(S)-NEA S)-NEA。