1-[Hexahydrocyclopenta[c]pyrrol-2(1H)-yl]-3-(4-methylbenzenesulfonyl)urea (Gliclazide) was synthesised over three steps from the starting material of cyclopentane-1,2-dicarboxylic anhydride. N-aminocyclopentane-1, 2-dicarboximide was obtained from the condensation reaction between the material and 80% hydrazine hydrate. The reduction of N-aminocyclopentane-1,2-dicarboximide and followed by the condensation with p-toluenesulfonyl urea generated Gliclazide. Every step was modified to be more simple and gave a 60% overall yield. The procedure is suitable for large-scale production.
