Ganciclovir Synthesis

9-[(l,3-Dihydroxy-2-propoxy)methyl] guanine (ganciclovir ) is an important antiviral nucleoside pharmaceutical structurally different from acyclovir. A novel method were studied, which used a N2,9-diacetylguanine to condense 2-acetoxymethoxy-l,3-dichloro-propane followed by acetylation and hydration processes.The compound 2-acetoxymethoxy-l,3-dichloropropane was synthesized as a starting material replacing a common 2-acetoxymethoxy-l,3-diphenylmethoxyl-propane. The yield of ganciclovir reached 77.4% compared with general 9.7%. And 2-acetoxymethoxy-l,3-dichloropropane was obtained in 62.2% yield with much bigger than 14.3% of yield in the preparation of 2-acetoxymethoxy -1,3-diphenylmethoxylpropane. It appears an economical practicability.Ganciclovir could be purified to more than 99.0%(HPLC) by a combination of acetone, acetic acid and water in 83.3% recovery as compared with 30% one when using water or methanol as solvent.