Expedient Synthesis of Rupatadine

Abstract

Rupatadine, a new potent, orally active dual antagonist of histamine and platelet‐activating factor (PAF), has been synthesized in 91% overall yield.

Keywords:

• 5‐methyl nicotonic acid
• 5‐methyl‐3‐chloromethyl pyridine hydrochloride
• rupatadine

Acknowledgment

The results reported here could not have been achieved without a team of experienced and hard working coworkers, who showed real commitment and dedication to the task.