Matsumoto H, Kaneko C, Yamada K, Takeuchi T, Mori T, Mizuno Y
Nucleic Acids Symp Ser. 1986(17):5-8.
In order to search for improved syntheses of 9-(2-hydroxyethoxymethyl) guanine and related antiviral agents, we tried several well documented general procedures (viz., fusion method) for the synthesis of N-glycosyl bond. Product distribution on alkylation of 4,5-disubstituted imidazoles as well as 2,6-disubstituted purines may depend upon the nature of alkylating agents (viz., 2-oxa-1,4-butanediol diacetate or 1-bromo-2-oxa-4-butanol acetate) and reaction conditions. A procedure for the synthesis of acyclovir and its N2-acetyl derivative could be improved to a considerable extent.
为了寻找9-(2-羟基乙氧基甲基)鸟嘌呤及相关抗病毒药物的改进合成方法，我们尝试了几种有充分文献记载的合成N-糖苷键的通用方法（即熔融法）。4,5-二取代咪唑以及2,6-二取代嘌呤烷基化时的产物分布可能取决于烷基化剂的性质（即2-氧杂-1,4-丁二醇二乙酸酯或1-溴-2-氧杂-4-丁醇乙酸酯）和反应条件。阿昔洛韦及其N2-乙酰衍生物的合成方法可以在很大程度上得到改进。
