Abstract

AbstractIn support of a program to develop a treatment for chemotherapy‐induced nausea and vomiting, two isotopically labeled forms of neurokinin‐1 receptor antagonist aprepitant have been synthesized. A [l4C]‐labeled version was synthesized for use in metabolism studies, while a [13C2,15N3]‐labeled version was synthesized for use in a study to determine the bioavailability of the final market image. Both syntheses utilized labeled chloroacetonitrile which was synthesized in two steps from labeled potassium cyanide. Copyright © 2004 John Wiley & Sons, Ltd.

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