脂肪酶在普瑞巴林制备中的应用进展

Application of Lipase in the Preparation of Pregabalin

目的对脂肪酶在普瑞巴林化学-酶法合成中的应用进行综述及探讨。方法通过文献检索及整理,综述了近年来在化学合成普瑞巴林的基础上引入脂肪酶拆分得到普瑞巴林手性中间体的应用进展,按脂肪酶的反应类型进行了分类,并对拆分2-乙氧羰基-3-氰基-5-甲基己酸乙酯得到普瑞巴林中间体的催化剂进行了阐述。结果脂肪酶催化拆分普瑞巴林中间体专一性强、产率高、环境友好。结论与单纯的化学法合成普瑞巴林相比,脂肪酶在普瑞巴林制备工艺中有明显的优势,具有良好的应用前景。

OBJECTIVE To review and discuss on the application of lipase in pregabalin chemoenzymatic synthesis. METHODS The paper summarized the application of lipase in the synthesis of the chiral intermediates by reviewing the literatures, and the lipase of resolving 2-carboxyethyl-3-cyano-5-methylhexanoic acid ethyl ester（CNDE）. RESULTS High selectivity, high yield, friendly environment on the lipase catalyzed resolution of pregabalin intermediate. CONCLUSION Compared with the chemical synthesis of pregabalin, lipase in preparation of pregabalin has obvious advantages in the process, it has a good application prospect.