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The syntheses of [14C] and [13C2,15N3]aprepitant

✍ Scribed by Charles S. Elmore; Dennis C. Dean; Yong Zhang; David G. Mellilo

Publisher
John Wiley and Sons
Year
2004
Tongue
French
Weight
133 KB
Volume
47
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

In 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 [^l4^C]‐labeled version was synthesized for use in metabolism studies, while a [^13^C~2~,^15^N~3~]‐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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