新型噻吩并四氢吡啶类化合物的合成及其抗血小板聚集活性  

Synthesis and Anti-platelet Aggregation Activities of Novel Thienopyridine Derivatives

作　　者：樊梦林 姜希明 刘颖[2] 刘登科[2] 王平保[2] 

机构地区：[1]天津医科大学研究生院,天津300193 [2]天津药物研究院有限公司,天津300193 [3]天津法莫西医药科技有限公司,天津300193

出　　处：《合成化学》2016年第4期297-301,共5页Chinese Journal of Synthetic Chemistry

基　　金：国家科技重大专项"重大新药创制"课题(2013ZX09102014)

摘　　要：噻吩并[3,2-c]四氢吡啶和噻吩并[2,3-c]四氢吡啶分别与取代苄溴(2a^2g)经取代反应后,用2 mol·L-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(3b^3e,3g和5a^5g);噻吩并[3,2-c]四氢吡啶酮与取代苄溴经取代反应,再与乙酸酐缩合,最后经2 mol·L-1氯化氢乙醚溶液成盐合成了噻吩并四氢吡啶衍生物(7d,7e,7g^7i)。3,5和7均为新化合物,其结构经1H NMR和ESI-MS表征。大鼠体内抗血小板聚集活性研究结果表明:3,5和7均有一定的抗血小板聚集活性,其中7d,7h和7i的抑制率分别为66.2%,86.8%和88.3%,活性优于阳性对照药噻氯匹啶。Novel reaction of tetrah thienopyridine derivatives（3b - 3e, 3g and 5a - 5g） were synthesized by substitution ydrothieno [ 3,2-c ] pyridine or tetrahydrothieno [ 2,3-c ] pyridine with substituted benzyl bromides, and salt forming reaction with ethereal hydrochloric acid. Novel thienopyridine derivatives （7d, 7e, 7g - 7i） were synthesized by substitution reaction of tetrahydrothieno [ 3,2-c ] pyridone with substituted benzyl bromides, and condensation with acetic anhydride, then salt forming with 2 mol · L^-1 ethereal hydrochloric acid. The structures were characterized by 1H NMR and ESI-MS. The results in platelet aggregation inhibition tests in vivo showed that the compounds exhibited certain activities, 7d, 7h and 7i showed better activities than the positive control drug ticlopidine, and the inhibitory rate were 66.2%, 86.8% and 88.3%, respectively.

关 键 词：噻吩并四氢吡啶衍生物 合成 抗血小板聚集活性 血栓 

分 类 号：O626[理学—有机化学] O621.3[理学—化学]