Studies on the synthesis of gimeracil

Objective To synthesize gimeracil,which is a potent dihydropyrimidine dehydrogenase inhibitor.Methods Gimeracil was synthesized by four steps from malononitrile,trimethyl orthoacetate and 1,1-dimethoxy-trimethylamine via condensation,cyclization,chlorination and hydrolysis reactions.Results Gimeracil was synthesized in overall yield of 65.6%,its structure was confirmed by MS,()~1H-NMR as well as elemental analysis.Intermediate compounds were confirmed by MS and()~1H-NMR.Conclusions The improved process has advantages of lower cost,mild reaction conditions,convenient work-up.It is suitable for industrial production.