Syntheses of morpholine-2, 3-diones and 2-hydroxymorpholin-3-ones: intermediates in the synthesis of aprepitant

…, KMJ Brands, B Craig, MA Huffman, JM McNamara

Index: Nelson, Todd D.; Rosen, Jonathan D.; Brands, Karel M.J.; Craig, Bridgette; Huffman, Mark A.; McNamara, James M. Tetrahedron Letters, 2004 , vol. 45, # 48 p. 8917 - 8920

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Citation Number: 18

Abstract

Aprepitant has recently been approved, in combination with other agents, as an effective treatment for preventing acute and delayed chemotherapy-induced nausea and vomiting (CINV) that can result from highly emetogenic chemotherapy in adults. 1 This is the first FDA-approved drug for the treatment of CINV that persists for more than 24 h after chemotherapy treatment. A core structural element of this h-NK1 receptor antagonist is an N-protected-2-hydroxymorpholin-3-one, ...