A Facile Synthesis of 1-(4-nitrophenyl)-3-morpholine-4-yl-5,6-dihydropyridin-2(1H)-one, A key Intermediate of Apixaban-An anticoagulant Drug

Abstract

Described herein is an improved synthesis of 1-(4-nitrophenyl)-3-morpholine-4-yl-5,6-dihydropyridin-2(1H)-one (1), a key intermediate for the synthesis of Apixaban. The present work provides robust and commercially viable manufacturing process for the synthesis of pure 1 with an overall yield of 48% over four steps and purity of around ≥ 98% by overcoming the limitations of the literature reported processes.