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

作者: Jérôme Keldenich , Audrey Denicourt-Nowicki , Christophe Michon , Francine Agbossou-Niedercorn

DOI: 10.1016/J.TET.2013.05.097

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

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