申请人:SUMITOMO PHARMACEUTICALS COMPANY, LIMITED
公开号:EP0204481A2
公开(公告)日:1986-12-10
A process for the production of optically active threo-3-(3,4-methylenedioxyphenyl)serine of formula:
which comprises subjecting racemic threo-3-(3,4-methylenedioxyphenyl) serine alkyl ester of formula:
wherein R is alkyl having 1 to 4 carbon atoms to optical resolution by using a resolving agent selected from the group consisting of optically active pyroglutamic acid and optically active dibenzoyltartaric acid in a solvent medium, separating the insoluble diastereomer salt, producing D or L-threo-3-(3,4-methylenedioxyphenyl)serine alkyl ester therefrom by treatment with an aqueous alkali, and then hydrolysing it to obtain
optically active threo-3-(3,4-methylenedioxyphenyl)-serine, which is useful as intermediate for producing optically active threo-3-(3,4-dihydroxyphenyl)-serine.
一种生产光学活性式苏-3-(3,4-亚甲二氧基苯基)丝氨酸的工艺:
其中包括将式......的外消旋苏氨酰-3-(3,4-亚甲二氧基苯基)丝氨酸烷基酯与式..:
其中 R 为具有 1 至 4 个碳原子的烷基,在溶剂介质中使用选自由光学活性焦谷氨酸和光学活性二苯甲酰酒石酸组成的组中的分解剂进行光学分解,分离出不溶性非对映异构盐,用水碱处理生成 D 或 L-硫代-3-(3,4-亚甲二氧基苯基)丝氨酸烷基酯,然后水解得到
光学活性苏氨酰-3-(3,4-亚甲二氧基苯基)丝氨酸,可作为生产光学活性苏氨酰-3-(3,4-二羟基苯基)丝氨酸的中间体。