2-二烷氨基-3-苯基-5-甲基-6-(1H-1,2,4-三唑-1-基)-噻吩并[2,3-d]嘧啶-4(3H)-酮衍生物的合成及其杀菌活性

Synthesis of 2-Dialkylamino-3-phenyl-5-methyl-6-(1H-1,2,4-triazol-1-yl)-thienopyrimidin-4(3H)-ones and Their Fungicidal Activities

用烯基膦亚胺与苯基异氰酸酯、仲胺的串联aza-Wittig反应合成了8个新的2-二烷氨基-3-苯基-5-甲基-6-(1H-1,2,4-三唑-1-基)-噻吩并[2,3-d]嘧啶-4(3H)-酮衍生物(6a^6h),其结构经1H NMR,MS和元素分析表征。初步生物活性测试结果表明,部分6表现出一定的抑菌活性,其中6f在浓度为5×10-5g.L-1时,对棉花炭疽菌的抑制率达到87%。

Eight novel 2-dialkylamino-3 -phenyl-5-methyl-6- （ 1H-1, 2,4-triazol-1 -yl ） -thieno [ 2,3 -d ] pyrimidin-4 （3H） -ones （6a ～6h） were synthesized via tandem aza-Wittig reaction of vinyliminophosphorane, phenyl isocynate and secondary amines. The structures were characterized by 1H NMR, MS and elemental analysis. The preliminary biological activity tests showed that 6 exhibited some fungicidal activities and 6f provided 87% inhibition activity against Colletotrichum gossypii at 5 x 10^-5 g . L^-1. Keywords： triazole ; thieno [ 2,3-d ] pyrimidin-4 （3H） -one; tandem aza-Wittig reaction ; synthesis; fungicidal activity