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Synthesis of a 14 C‐labeled FPTase inhibitor via a Pd‐catalyzed cyanation with Zn( 14 CN) 2 and via bromo[ 14 C]acetic acid
Author(s) -
Ho Jonathan Z.,
Elmore Charles S.,
Braun Matthew P.
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.1545
Subject(s) - cyanation , chemistry , catalysis , ring (chemistry) , piperazine , stereochemistry , medicinal chemistry , radiochemistry , organic chemistry
14 C‐Labeled farnesyl‐protein transferase inhibitor 1a was required for drug metabolism studies. The first approach was to synthesize 14 C‐labeled 1b using Zn( 14 CN) 2 in a Pd‐catalyzed cyanation. A second approach was to prepare labeled 1c with the 14 C‐label in the piperazine ring. All metabolites from 1b were non‐radioactive whereas the same metabolites from 1c were all radioactive and quantifiable. Copyright © 2008 John Wiley & Sons, Ltd.