【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。更多还原

【Abstract】 Novel thienopyridine derivatives( 3b ~ 3e,3g and 5a ~ 5g) were synthesized by substitution reaction of tetrahydrothieno[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- 1ethereal hydrochloric acid. The structures were characterized by1 H 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.更多还原