抗病毒药物缬更昔洛韦的合成研究

Synthesis of anti-viral agent valganciclovir

目的探索更简便的合成缬更昔洛韦的工艺路线,为进一步研究开发提供基础。方法以更昔洛韦为原料,经过酯化、还原两步反应得到目标物缬更昔洛韦。结果实验路线简便,总收率达到20%。结论本文探索了简便的缬更昔洛韦合成工艺,确立了比较合理的酯化条件,改进了氢化脱保护基条件,为将该工艺用于中试放大提供了依据。

Objective To explore a simple synthetic route of valganciclovir for its further development. Method Valganciclovir was synthesized through esterification and hydrogenation, using ganciclovir as starting material. Results The total yield was above 20%. Conclusions It is feasible to synthesize valganciclovir using ganciclovir as starting material through esterification and with the modified deprotection method by (hydrogenation). The proposed method could be used for large-scale preparation of valganciclovir.