酶促萘普生酯的选择性水解拆分  

Resolution of Racemic Naproxen Ester by Enantioselective Hydrolysis Catalyzed by Lipase

作　　者：崔玉敏[1] 魏东芝[1] 周文瑜[1] 俞俊棠[1] 

机构地区：[1]华东理工大学生物反应器工程国家重点实验室,上海200237

出　　处：《华东理工大学学报（自然科学版）》2001年第2期121-123,134,共4页Journal of East China University of Science and Technology

基　　金：国家自然科学基金! (2 970 60 0 3 ) ;华东理工大学生物反应器工程国家重点实验室开放课题部分资助

摘　　要：柱状假丝酵母脂肪酶可以选择性催化 S-萘普生甲酯、乙酯和乙氧基乙基酯发生水解 ,从而对化学合成的混旋萘普生进行拆分 ,制备具有高光学纯度的 S-对映体。利用中等极性大孔吸附树脂 HZ- 80 6作为固定化载体 ,可在酶分子周围营造一个有利于反应的微环境 ,有效地提高酶的催化活力及解决酶的回收。在中等极性大孔吸附树脂固定化酶填充床反应器中 ,混旋乙氧基乙基萘普生酯可被连续水解拆分 ,当流量为 72 m L/h时 ,酯的水解率为 1 7% ,光学纯度为 89.1 %Chemically synthesized racemic naproxen was resolved by biological method and optically pure S enantiomer was prepared. Lipase from Candida cylindracea was able to catalyze the hydrolysis of methyl, ethyl and ethoxyethanol naproxen ester effectively and enantioselectively. S enatiomer was obtained by separation from remained ester. As a carrier, HZ 806, the porous adsorption resin with middle polarity can make a micro circumstance helpful to hydrolysis around enzyme molecules. Enzyme activity was improved and enzyme could be recycled easily with immobilization on HZ 806. Racemic ethoxyethanol naproxen ester could be resolved by hydrolyzing continuously in packed bed reactor with lipase immobilized on HZ 806. S naproxen with 89.1% optical purity was obtained.

关 键 词：对映体选择性水解 萘普生 脂肪酶 固定化脂肪酶填充床反应器 

分 类 号：R971.1[医药卫生—药品] Q814[医药卫生—药学]