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Syntheses of AZ12320927 labeled with H‐3, C‐14, and H‐2
Author(s) -
Elmore Charles S.,
Powell Mark E.,
Heys J. Richard
Publication year - 2008
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.1534
Subject(s) - chemistry , tritium , specific activity , radiochemistry , hydrogen isotope , hydrogen , nuclear chemistry , combinatorial chemistry , organic chemistry , enzyme , physics , nuclear physics
In support of a program to develop a treatment for depression, three isotopically labeled forms of the 5‐HT 1B antagonist AZ12320927 were synthesized. A tritium labeled version was synthesized for autoradiography using Ir‐catalyzed hydrogen–tritium exchange. A C‐14 labeled version was prepared for use in metabolism studies in four‐steps from [ u‐ 14 C] p ‐nitrophenol. A stable isotope labeled version was synthesized for use as an internal standard for LC/MS/MS quantitation in two steps from chromenone 1. Copyright © 2008 John Wiley & Sons, Ltd.