N-取代-2-{4,5,6,7-四氢噻吩并[3,2-c]吡啶-5-基}乙酰胺的合成及其抗血小板聚集活性  

Synthesis of N-substituted-2{4,5,6,7-tetrahydrothienopyridine-5-yl}acetamides and Their Anti-platelet Aggregation Activities

作　　者：支爽[1] 郑帼[2] 刘冰妮[3] 王景阳[3] 刘登科[3] 

机构地区：[1]天津工业大学环境与化学工程学院,天津300160 [2]天津工业大学天津市纺织纤维界面处理技术工程中心,天津300160 [3]天津药物研究院天津市新药设计与发现重点实验室,天津300193

出　　处：《合成化学》2012年第3期312-315,共4页Chinese Journal of Synthetic Chemistry

基　　金：国家"重大新药创制"科技重大专项项目(2009ZX09103-078);天津市科技计划项目(09ZCKFSH01300)

摘　　要：以4,5,6,7-四氢噻吩并[3,2-c]吡啶盐酸盐和2-氧代-2,4,5,6,7,7a-六氢噻吩并[3,2-c]吡啶盐酸盐为起始原料,合成了9个未见文献报道的ADP受体拮抗剂——N-取代-2-{4,5,6,7-四氢噻吩并[3,2-c]吡啶-5-基}乙酰胺(1a～1e,2a～2d),收率61.4%～80.3%,其结构经1H NMR和HR-MS表征。大鼠体内抗血小板聚集活性研究表明,1和2均有一定的抗血小板聚集作用,其中1d和2d的作用较强,抑制效率分别为50.0%和58.9%,且2d的抑制作用优于阳性对照药噻氯匹定。Nine novel ADP receptor inhibitors, N-substituted-2- { 4,5,6,7-4,5,6,7-tetrahydrothieno [ 3,2-c] pyridine-5-yl } acetamides（ 1a - le, 2a - 2d）, were synthesized from 4,5,6,7-tetrahydrothieno[3,2-c] pyridine hydrochloride and 2-oxo-2,4,5,6,7 ,Ta-hexahydrothieno[ 3,2-c] pyridine hydrochloride in yields of 61.4% - 80.3%. The structures were characterized by 1H NMR and HR-MS. The anti-plated aggregation activities were evaluated by plated aggregation inhibition tests in rats. The results showed that 1 and 2 exhibited certain anti-platelet aggregation activities, in which the inhibitions of ld and 2d were 50.0% and 58.9%, respectively. The inhibition of 2d was better than the positive control of ticlopidine.

关 键 词：噻吩并吡啶 ADP受体拮抗剂 抗血小板聚集 酰胺 药物合成 

分 类 号：O625.63[理学—有机化学] R914.5[理学—化学]