木瓜蛋白酶催化的不对称杂环酮的醇醛缩合反应研究

Papain-Catalyzed Asymmetric Aldol Reactions of Heterocyclic Ketones with Aldehydes

采用木瓜蛋白酶多功能性催化不对称杂环酮与芳香醛之间的醇醛缩合(Aldol)反应。通过对溶剂、含水量、投料比、酶载量以及反应温度等条件的筛选,发现木瓜蛋白酶在该反应体系中展示了较好的催化活性和底物适应性。在优化反应条件下,获得了最高37%的产率和78%的ee值。本文报道的木瓜蛋白酶在有机溶剂中具有类似天然醛缩酶的催化功能。

The new promiscuous activity of papain has been observed to catalyze the direct asymmetric Aldol reaction of heterocyclie ketones with aromatic aldehydes. We studied the effects of solvent, water content, ratio of substrates, enzyme loading and temperature on the reaction. Papain showed favorable catalytic activity and had a good adaptability to different substrates in the reaction. Up to 37% yield and 78% ee were achieved under optimal conditions. It is interesting that papain possesses the function of aldolase in organic solvents.