阿昔洛韦琥珀酰亚胺活性酯的制备研究

Synthesis of acyclovir succinimide active ester

目的合成阿昔洛韦琥珀酰亚胺活性酯。方法以阿昔洛韦为起始原料,在二甲基甲酰铵(DMF)为溶媒及三乙胺的碱性条件下,与丁二酸酐反应生成阿昔洛韦衍生物9-(2-丁二酸单酰乙氧基甲基)鸟嘌呤(SACV),再与N-羟基琥珀酸亚胺在N,N-二环己基碳化亚胺的存在条件下合成阿昔洛韦琥珀酰亚胺活性酯。结果与结论合成产物产率为79.1%,mp为125～126℃,其结构经IR和NMR确证,所得化合物为一新化合物。

Objective To synthesize acyclovir succinimide ester. Methods Title compound was prepared by acyclovir （ 1 ） which was coupled with succinic anhydride in the present of triethylamine and DMF, to afford acyclovir＇s derivatives [ 9-（ 2-single acidated butanedioic acid ethoxyl methyl） guanine ] （2）. The compound （2） was coupled with N-hydroxysuccinimide （3） in the presence of DCC to afford title compound （4）. Results and ConclusionThe title compound was synthesized. The title compound was confirmed by NMR and IR, the yield was 79.1%, and mp was 126 ℃ ,which was a new compound.