A Scalable and Facile Process for the Preparation of N-(Pyridin-4-yl) Piperazine-1-Carboxamide Hydrochloride. (March 2016) - Wei, Daiyan
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.