三组分反应高效合成1,2,4-三唑烷类化合物

A Straightforward Approach to Synthesizing 1,2,4-triazoles via Three-Component Reaction

β,γ-不饱和酮酸酯,L-苯丙氨酸和偶氮二甲酸二异丙酯通过原位生成不饱和甲亚胺叶立德,再发生1,3-偶极环加成反应,高效获得多取代的1,2,4-三唑烷衍生物(60%-88%的收率,大于20∶1的非对映选择性).

A general, straightforward three-component synthesis of 1,2,4-triazole alkyl derivatives from β, γ-unsatu- rated ct-ketoesters, L-phenylalanine and （Z）-diisopropyl diazene-1,2-dicarboxylate via 1,3-dipolar cycloaddition of azomethine ylides generated in situ has been developed. The simple method provides diverse products in good yields （60% -88% ） with good diastereoselectivities （up to 20：1 dr）.