Studies On A New Antihypertention Drug OPC-21268

The mechanisms of hypertention and the development of the antihypertention drugs were briefly described in this paper. OPC-21268, an orally effective, nonpeptide arginine vasopressin V1 receptor antagonist was introduced. Benzylamine as the starting material, a 12 steps synthetic route was devised .And the synthetic process was studied. The structures of OPC-21268 and several intermediates were identified by 1H-NMR or MSThe yield of l-benzyl-4-piperidone was increased by 9.5% and the cost was reduced after modifying the process. Several factors including the ratio of start materials, solvent, time, temperature were investigated to optimize the Friedel-Crafts reaction. Two methods were applied to debenzylate simply at standard pressure.