Candidarugosa脂肪酶二次拆分制备(S)-萘普生

Candida rugosa Lipase-catalyzed Double Resolution for the Preparation of (S)-Naproxen

用柱状假丝酵母脂肪酶(CRL)对外消旋萘普生甲酯进行手性水解拆分,所得(S)-萘普生粗品经酯化后,继续用CRL进行第二次拆分得到(S)-萘普生。根据建立的理论曲线,在第一次和第二次拆分转化率分别为46.8%和75.1%时终止反应,以31.8%的产率获得了ee值大于99%的(S)-萘普生。

（S） -Naproxen was obtained from naproxen methyl ester via asymmetric hydrolysis catalyzed by Candida rugosa lipase （CRL） to give crude （S） -naproxen, then esterification with methanol and further hydrolysis by CRL catalyzed. According to the established theoretical curves, when the conversions of the first and second resolution were 46.8 % and 75.1%, respectively, （S） -naproxen was obtained with an overall yield of 31.8 % and the value ofee over 99 %.