Efficient Synthesis of Deuterium-Labelled Ganciclovir-d5 and Its Prodrug Valganciclovir-d5

An efficient protocol has been developed for the synthesis of deuterium labeled ganciclovir-d5, a potent anti-cytomegalovirus agent and its prodrug, valganciclovir-d5, by using inexpensive and commercially available glycerol-d5 reagent. Structure and purity of the synthesized compounds are confirmed by 1H NMR and MS spectral data. The deuterium incorporation in ganciclovir-d5 and its prodrug was >98% which resembles the reported earlier deuterium abundance in the labeled starting material (glycerol-d5, >98% atom D). The results indicate that there is no loss of deuterium by exchange in the course of synthesis. Hence, these molecules can be used as standards in bio-analytical studies.