论文部分内容阅读
以鸟嘌呤核苷(1)为原料,经羟基保护得到2’,3’,5’-三-O-乙酰基鸟嘌呤核苷(2),2与三氯氧磷反应得到2-氨基-6-氯-9-(2’,3’,5’-三-O-乙酰基-β-D-呋喃核糖)嘌呤(3),3经重氮化、水解和O-烷基化得到2-烷氧基-6-氯-9-(2’,3’,5’-三-O-乙酰基-β-D-呋喃核糖)嘌呤(4a～4c),4a～4c经胺解和水解脱保护反应得到12个未见报道的N6-烷基-2-烷氧基腺苷化合物5a～5c.化合物的结构经1H NMR,13C NMR,IR和HRMS等得到表征,同时对合成的N6-烷基-2-烷氧基腺苷化合物进行了抗血小板凝集活性测试.结果表明,在测试浓度为100μmol/L时,N6-(4-甲基苄基)-2-苄氧基腺苷(5c3)和N6-(2-苯乙基)-2-苄氧基腺苷(5c4)具有相对较低的聚集率,具有一定的抗血小板凝集活性.
Using guanosine (1) as starting material, 2 ’, 3’, 5’-tri-O-acetylgoguanosine (2) is obtained by hydroxyl protection and 2 is reacted with phosphorus oxychloride to obtain 2-amino- Diazotization, hydrolysis and O-alkylation of 6-chloro-9- (2 ’, 3’, 5’-tri-O-acetyl-β-D-ribofuranosyl) purine (3) (4a-4c), 4a-4c After amineysis and water 12 unaffected N6-alkyl-2-alkoxy adenosine compounds 5a ~ 5c were obtained by the deprotection reaction.The structures of the compounds were characterized by 1H NMR, 13C NMR, IR and HRMS etc. Meanwhile, the synthesized N6- Alkyl-2-alkoxy adenosine compounds were tested for anti-platelet aggregation activity.The results show that at the test concentration of 100μmol / L, N6- (4-methylbenzyl) -2-benzyloxy adenosine 5c3) and N6- (2-phenethyl) -2-benzyloxyadenosine (5c4) have a relatively low aggregation rate and have certain anti-platelet aggregation activity.