Synthesis of Antipsychotic Drug, Cariprazine: An Improved and Commercially Viable Synthetic Approach

The novel synthetic route to the antipsychotic drug Cariprazine was developed and demonstrated on a commercial scale. The synthesis of Cariprazine is achieved from N-(4- oxocyclohexyl) acetamide by using various reactions such as Wittig-Horner reaction, reduction of alkene, hydrolysis of ester, deacylation, amidation, reduction of Weinreb amide to yield the corresponding aldehyde, and finally reductive amination of aldehyde in the presence of the corresponding amine to form Cariprazine. In this article, we report a novel intermediate 2-[trans-4- (3,3-Dimethylureido)cyclohexyl]-N-methoxy-N-methyl acetamide by avoiding potentially genotoxic substances/intermediates, tedious, drastic reaction conditions.