Preparation of chiral key intermediates of morpholine based neurokinin receptor antagonists by asymmetric allylic alkylation

The preparation of optically active morpholine-2-aryl-2-allyl derivative from morpholine-2-aryl-3-ones is reported. The optically active tetrasubstituted stereocenter is introduced during a palladium promoted asymmetric allylic alkylation. The resulting compounds are useful intermediates in the synthesis and development of potent NK antagonists.