酶法水解在消旋体拆分中的应用  

Resolution of Racemate by the Hydrolysis with Enzyme

作　　者：谢娜[1] 罗智[2] 项光亚[2] 林菊生[1] 

机构地区：[1]华中科技大学同济医学院附属同济医院肝病研究所,武汉430030 [2]华中科技大学同济医学院药学院药物化学系,武汉430030

出　　处：《华中科技大学学报（医学版）》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)

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 βObjective 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.

关 键 词：洛尔类β-受体阻滞剂 中间体 消旋体 酶法水解 

分 类 号：TQ463.4[化学工程—制药化工]