α-(1H-1,2,4-三唑-1-基)-β-芳胺基丙烯腈的合成及生物活性

SYNTHESIS AND BIOLOGICAL ACTIVITIES OF α-(1H-1,2,4-TRIAZOL-1-YL)-β- ARYLAMINACRYLONITRILE

利用芳胺与中间体 α-( 1 H-1 ,2 ,4 -三唑 -1 -基 ) -β-二甲氨基丙烯腈盐酸盐 ( 2 )的亲核取代反应 ,合成了一系列目标化合物α-( 1 H-1 ,2 ,4 -三唑 -1 -基 ) -β-芳胺基丙烯腈 ( 3a-3r) ,所有化合物均经元素分析和 1 H NMR确定 ,由1 HNMR分析结果推断为 E式构型 .初步生物活性测定结果表明 ,部分化合物有一定的杀菌活性 .

A series of α-(1H-1,2,4-triazol-1-yl)-β-arylaminacrylonitrile 3a-3r were synthesized in good yield by the nucleophilic reaction of arylamines with α-(1H-1,2,4-triazol-1-yl)-β-dimethylamino-acrylonitrile hydrochloride 2. Their structures were confirmed by means of elemental analysis and 1H NMR, and E configurations were drawn from the data of 1H NMR. The preliminary bioassay results indicated that some of these compounds possessed fungicidal activities.$$$$