Research on the Improved Synthetic Process to Revefenacin

OBJECTIVE  To explore and optimize the synthetic process to revefenacin.

METHODS Revefenacin(1) was prepared using 2-phenylbenzoic acid(15) and N-Boc-4-hydroxypiperidine(3) as starting material through 4 steps including Curtius rearrangement, nucleophilic substitution, hydrogenation and condensation.

RESULTS The yield of this synthetic process of revefenacin was 63.4%, and its structure was confirmed by HRMS, ¹H NMR, and ¹³C NMR.

CONCLUSION This synthetic route has the advantages of easily available raw materials, high yield, simple operation, and environmental friendliness, making revefenacin suitable for industrial production.