关键词: 腺苷, N⁶-烷基-2-烷氧基腺苷, 合成, 结构表征, 抗血小板凝集

Guanosine (1) as the starting material was protected by acetic anhydride to get 2,3,5-tri-O-acetyl-guanosine (2), then chlorinated with phosphorus oxychloride to obtain 2-amino-6-chloro- 9-(2,3,5-tri-O-acetyl-β-D-ribofuranosyl)purine (3). Compound 3 was diazotized and hydrolyzed, subsequently reacted with several alkyl halides respectively to afford 2-alkoxy-6-chloro-9-(2,3,5-tri-O-acetyl-β- D-ribofuranosyl)purine (4a～4c). 2-Alkoxy-N⁶-alkyl adeno-sine compounds 5a～5c were acquired by aminolysis and deprotection reaction of compounds 4a～4c. All compounds 5a～5c have not been reported so far. The structures of compounds 5a～5c were identified by ¹H NMR, ¹³C NMR, IR and HRMS techniques. What is more, the anti-platelet aggregation rates for the final compounds were measured. At a concentration of 100 μmol/L, the test results of the biological activity of anti-platelet aggregation showed that N⁶-(4-methylbenzyl)-2-benzyloxy adenosine (5c₃) and N⁶-(2-phenethyl)-2-benzyloxy adenosine (5c₄) have a relatively low aggregation rate and have a certain anti-platelet aggrega-tion activity.

Key words: adenosine, 2-alkoxy-N⁶-alkyl adenosine, synthesis, characterization, anti-platelet aggregation