摘要
目的 用特定的酶的不对称水解作用制备洛尔类 β 受体阻滞剂合成的重要中间体原料—S (- ) 2 ,3 二溴丙醇醋酸酯。方法 采用生物有机合成方法 ,应用手性试剂胰酶 ,对消旋体 (± ) 2 ,3 二溴丙醇醋酸酯进行拆分。结果 水解得到了S (- ) 2 ,3 二溴丙醇醋酸酯。结论 酶法水解用于消旋体的拆分为制备洛尔类 β
Objective A specifical enzyme was used for the enantioselective hydrolysis of (±)-1-acetoxy-2, 3-dibromopropane. Methods According to the biological organic chemistry, pancreatin was used to hydrolyze (±)-1-Acetoxy-2,3- dibromopropane asymmetrically. Results (s)-1 was prepared successfully. From (s)-1, we can prepare the optically pure (s)-isomer of the typical β-adrenergic blocking agents. Conclusion Resolution of racemate by the hydrolysis with enzyme provides a brand-new method for the preparation of β-adrenergic blocking agents.
出处
《华中科技大学学报(医学版)》
CAS
CSCD
北大核心
2003年第3期289-290,共2页
Acta Medicinae Universitatis Scientiae et Technologiae Huazhong
基金
国家自然科学基金资助项目 (No 39970 85 8)