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.pdfVIP

Journal of Organic Chemistry Research 有机化学研究, 2018, 6(4), 87-94 Published Online December 2018 in Hans. /journal/jocr /10.12677/jocr.2018.64013 Studies on Synthesis and Biological Activities of 2,7-Diamino Substituted Thienopyrimidinone Derivatives Shuoxing Xu, Shengzhen Xu* College of Science, Huazhong Agricultural University, Wuhan Hubei th th th Received: Nov. 5 , 2018; accepted: Nov. 20 , 2018; published: Nov. 27 , 2018 Abstract 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 con- firmed 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. Keywords Thienopyrimidinone Derivatives, Aza-Wittig Reaction, Synthesis, Antibacterial Activity 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 徐硕星，徐胜臻* 华中农业大学理学院，湖北 武汉 收稿日期：2018年11月5 日；录用日期：2018年11月20 日；发布日期：2018年11月27 日 *通讯作者。 文章引用: 徐硕星, 徐胜臻. 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[J]. 有机化学研究, 2018, 6(4): 87-94. DOI: 10.12677/jocr.2018.64013 徐硕星，徐胜臻 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 1 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，H 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