NEW PRODUCTION ROUTE FOR N-MONOACYLPIPERAZINE

摘要

PROBLEM TO BE SOLVED: To obtain the subject novel N-monoacylpiperazine in high yield by effecting the N-acylation reaction in the presence of two NH groups without the N-protection of one NH group in the (homo)piperazine by allowing specific two compounds to react with each other. SOLUTION: (A) A compound of formula I (n is 2, 3) and (B) a compound of formula II [R1 is a (substituted) lower alkyl, a (substituted) aryl, a (substituted) heterocyclic ring; R2 is a (substituted) aryl] are allowed to react with each other in a solvent with heat under pressure to give a compound of formula III. Etyl acetate, toluene, acetonitrile, dioxane, tetrahydrofuran and the like can be used as a solvent. This production process can be utilized as an industrial production process for N-monoacyl(homo)piperazine and a part of production process for manufacturing the medicines having this chemical skeleton.