一种新型含氟三氮唑取代噻吩并嘧啶酮的合成

Synthesis of A New Fluorine Containing Triazole Substituted Thieno Pyrimidine Ketone

利用Gewald反应,关环生成噻吩,产物同PPh3、C2Cl6、Et3N作用得到膦亚胺,再用对氟苯基异氰酸酯与之作用得到碳二亚胺,碳二亚胺与一种伯胺反应得到2-(2-羟基乙基)胺-3-对氟苯基-5-甲基-6-(1H-1,2,4-三唑-1-基)-噻吩并[2,3-d]嘧啶-4(3H)-酮。其结构经1H NMR,MS和元素分析表征。生物活性测试表明,此种含氟衍生物对农作物病菌部分菌体有较大的抑制作用,其中对棉花枯萎菌达到90%的抑制率,对其它五种作物病菌也达55%以上的抑制率。

To produce thieno through Gewald reaction and then with which reacts PPh3, C2Cl6, Et3N to produce lminophosphorane, then react with 4-Fluorophenyl Isocyanate and Primary Amine to produce some new materials： 2-（2- hydroxyethyl ） amine-3 - （ 4 -fluorophenyl ） - 5 - methyl - 6 - （ 1 H- 1,2,4 - Triazol - 1 - yl ） - thieno [ 2,3 - d ] pyrimidin - 4 （3H）-Ketone （5）. The structures were confirmed by 1H NMR, MS techniques and elemental analyses. The biological activity tests showed that some of them exhibited a strong inhibiting effect upon crop biomasses and provided 90% inhibition activity against Cotton Fusarium Wilt, as to other five bacteria, over 55%.