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The syntheses of [ 14 C] and [ 13 C 2 , 15 N 3 ]aprepitant
Author(s) -
Elmore Charles S.,
Dean Dennis C.,
Zhang Yong,
Mellilo David G.
Publication year - 2004
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.872
Subject(s) - aprepitant , chemistry , radiochemistry , bioavailability , vomiting , antagonist , tachykinin receptor 1 , stereochemistry , nuclear chemistry , medicinal chemistry , pharmacology , receptor , antiemetic , substance p , biochemistry , medicine , neuropeptide
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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