Efficient one-pot process for synthesis of antiviral drug Ganciclovir

Abstract

A regioselective novel one-pot synthesis of heterocyclic purine derivative antiviral agent Ganciclovir in which initially guanine is treated with acetic anhydride in the presence of iodine (5%) to get diacetyl guanine intermediate, which undergoes in situ N-alkylation with AMDP in presence of catalytic acidic Amberlite IR-120 to get N-alkylated intermediate and finally deacetylation to get pure regioselective Ganciclovir, which is commercially viable and eco-friendly.

Graphical abstract

We developed one-pot synthesis of antiviral drug Ganciclovir. Initially, Guanine is treated with acetic anhydride and iodine to yield diacetyl guanine 3. This intermediate then reacted with AMDP in the presence of acidic Amberlite IR-120 to obtain compound 5. Finally, deacetylation yields Ganciclovir 1, a commercially viable and eco-friendly process.