关键词: α-腺嘌呤阿拉伯糖苷;, 无溶剂, 微波辐射, 无催化剂

Abstract:

In order to develop the efficient synthesis of α-adenine arabinoside, the key intermediate 9-α-D-(2',3',5'-tri-O-acetyl)-6-chloropurineside was obtained in 85% yield from the condensation of 6-chloropurine and 1,2,3,5-tetra-O-acetatyl-β-D-arabinose under solvent- and catalyst-free conditions with microwave irradiation. α-Adenine arabinoside was synthesized from the intermediate via deacetylation catalyzed by Na₂CO₃, followed by aminolysis in saturated NH₃/CH₃OH in one pot. The intermediate was obtained in consist yield even on a 100 g scale. The analogues α-2-fluoroadenine arabinoside and α-2-aminoadenine arabinoside were obtained via similar method.

Key words: α-adenine arabinoside;, solvent-free, microwave irradiation, metal-free