有机溶剂-水双液相体系脂肪酶不对称水解合成S-(+)-萘普生

Synthesis of S (+) Naproxen by Lipase Asymmetric Hydrolysis in an Aqueous Organic Solvent Biphase System

采用有机溶剂－水双液相体系作为反应介质，并用键合有—Ｃ６Ｈ５的无定型多孔硅胶作为分散剂增大两相间的接触面，用圆柱状假丝酵母脂肪酶对萘普生甲酯进行不对称水解．考察了酶浓度、体系ｐＨ值、温度、分散剂对反应的影响．当转化率为２４．３％时，产品萘普生的对映体过量值（ｅｅ）为９４．９％，剩余底物萘普生甲酯的对映体过量值（ｅｅ）为３０．５％，当以异辛烷作为有机相时，该体系酶催化水解的对映体比率（Ｅ）约为５０．

The enzymatic resolution of ( R,S ) naproxen was accomplished by treatment of naproxen methyl ester in an aqueous organic solvent biphase system with a number of commericially available Candida rugosa lipase. The effects of lipase concentration, dispersing agent, temperature and pH value on reaction conversion have been studied. With isooctanes as organic phase,0.2 mol/L phosphate buffer as aqueous phase and 2%YWG C 6H 5 as dispersing agent, 94.9% enantiomeric excess could be obtained at 24.3% conversion of naproxen methylester.