A scalable and facile process for the preparation of N-(pyridin-4-yl)piperazine-1-carboxamide hydrochloride

作者：Wei, Daiyan; Chen, Ligong; Yan, Xilong; Li, Yang; Li, Jianye; Wang, Donghua^*

来源：Journal of Chemical Research, 2016, 40(3): 152-155.

DOI：10.3184/174751916X14546711471143

• N-(pyridin-4-yl)piperazine-1-carboxamide hydrochloride
• Rho kinase inhibitor
• asymmetric urea
• N,N '-carbonyldiimidazole

A scalable and facile synthetic process for N-(pyridin-4-yl)piperazine-1-carboxamide hydrochloride, a novel Rho kinase inhibitor with an unsymmetrical urea structure currently under investigation for the treatment of central nervous system disorders, was established. After optimisation of the reaction conditions, N-(pyridin-4-yl)piperazine-1-carboxamide hydrochloride was synthesised from 4-aminopyridine and N,N'-carbonyldiimidazole through acylation, deprotection and salt formation. This new procedure affords the product in 53% overall yield with high purity and it can be easily scaled up for production.

• 出版日期2016-3
• 单位天津大学