抗病毒药阿昔洛韦的合成改进

The synthesis of antiviral drug Acyclovir

鸟嘌呤、六甲基二硅氮烷和 (NH4 ) 2 SO4 回流反应 1 8h,浓缩 ,溶于苯 ,过滤后与 Ac OCH2 CH2 OCH2 Br在 Hg(CN) 2 的催化作用下缩合 ,水解得 9-[(2 -乙酰氧乙氧基 )甲基 ]鸟嘌呤 (1 ) ,1最后与 CH3 NH2 反应制得阿昔洛韦。总收率为72 .3 %。

The mixture of guanine,HN(SiMe 3) 2 and (NH 4) 2SO 4 was refluxed for 18h and evaporated.The residue was taken up in C 6H 6,filtered and condensated with AcOCH 2CH 2OCH 2Br in the presence of the catalyst Hg(CN) 2.The condensation mixture were hydrolyzed to give 9 (2 acetoxyethoxymethyl) guanine(1).1 reacted with MeNH 2 to give Acyclovir.The overall yield was 72.3%.