Synthesis of a Chiral Key Intermediate of Neurokinin Antagonist SSR 240600 by Asymmetric Allylic Alkylation
Abstract
The preparation of optically active morpholine-2-aryl-2-acetaldehyde from morpholine-2-aryl-3-one is reported. The quaternary carbon is introduced during a palladium-promoted asymmetric allylic alkylation. This is a useful intermediate in the synthesis and development of potent NK antagonist.