2,7-二氨基取代噻吩并嘧啶酮衍生物的合成与生物活性研究  

Studies on Synthesis and Biological Activities of 2,7-Diamino Substituted Thienopyrimidinone Derivatives

作　　者：徐硕星 徐胜臻[1] Shuoxing Xu;Shengzhen Xu(College of Science,Huazhong Agricultural University,Wuhan Hubei)

机构地区：[1]华中农业大学理学院,湖北武汉

出　　处：《有机化学研究》2018年第4期87-94,共8页Journal of Organic Chemistry Research

摘　　要：噻吩并嘧啶酮类衍生物由于其良好的生物活性和药理活性,在医学和农用化学领域有很广阔的应用前景。利用三组分aza-Wittig反应,用3,4-二乙氧羰基-2,5-双三苯基膦亚胺噻吩、芳基异氰酸酯、亲核试剂胺或水合肼以54%~64%的收率合成了12个未见文献报道的化合物,通过IR,1H NMR,LC-MS对化合物进行了表征。进一步探究了化合物的抑菌活性,结果表明部分化合物对茶树生赤霉菌和茶树生茎点霉有良好的抑菌活性。Thienopyrimidinone derivatives have wide application prospect in the field of medicine and agri-cultural chemical due to their good biological and pharmacological activities. 12 new compounds which have not been reported in the literature were synthesized in 54% - 64% yields via aza-Wittig reaction of 3,4-diethoxy-2,5-bis(triphenylphosphine)phosphinimine thiophene with aromatic iso-cyanate and nucleophile amine or hydrazine hydrate;the new compounds were confirmed by IR, 1H NMR, LC-MS. Their antibacterial activities were tested and some of the compounds showed good antibacterial activity to gibberella of tea and phoma of tea.

关 键 词：噻吩并嘧啶酮衍生物 AZA-WITTIG反应 合成 抑菌活性 

分 类 号：O6[理学—化学]