A practical synthesis of 7-ethyl-octahydro-2-methyl-6H-pyrazino-[1,2-c]pyrimidin-6-one (Centperazine), an anti-filarial drug

摘要

7-Ethyl-octahydro-2-methyl-6H-pyrazino[1,2-c]pyrimidin-6-one (Centperazine) 1, an anti-filarial drug, currently undergoing phase 111 clinical trials has been synthesized by a short, practical and economical route suitable for large scale production. Thus 2-(2-ethylaminoethyl)pyrazine obtained from 2-vinylpyrazine and ethyl amine, on ethoxycarbonylation, catalytic hydrogenation, cyclo carbamation and N-methylation yields Centperazine 1 in 23.1% overall yield.