脂肪酶催化Michael加成反应合成苄丙酮香豆素抗凝血剂及其衍生物

Synthesis of warfarin anticoagulant and its derivatives through Michael addition catalyzed by lipase

以含水有机溶剂作为反应介质,以爪哇毛霉的天野脂肪酶M作为生物催化剂,利用4-羟基香豆素和α,β-不饱和酮的Michael加成反应,经一步催化合成了抗凝血剂苄丙酮香豆素及其衍生物;考察了反应条件对产物收率的影响.结果表明,该合成路线反应条件温和,产物收率高,有一定的实际应用意义.

Amano li chael addition of 4 pase M from mucor javanicus was used as a biocatalyst to catalyze the Mi hydroxycoumarin to α ,β-unsaturated enones in organic medium in the pres ence of water yielding warfarin anticoagulant and derivatives via one step. The effects of reac tion conditions on the yield of the target product were examined. Results indicate that the pres ent approach is characterized by mild reaction condition and high yield of target product, show ing potential in practical applications.