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Synthesis of a tritium‐labeled photo‐affinity probe based on an atypical leukotriene biosynthesis inhibitor
Author(s) -
Kumar Nag S.,
Braun Matthew P.,
Chaudhary Ashok G.,
Young Robert N.
Publication year - 2011
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.1804
Subject(s) - chemistry , tritium , biosynthesis , thiazole , triethylamine , anhydrous , radiosynthesis , stereochemistry , combinatorial chemistry , biochemistry , organic chemistry , enzyme , physics , microbiology and biotechnology , in vivo , nuclear physics , biology
A radiolabeled photo‐affinity probe containing a diazirine group was designed and synthesized based on an atypical leukotriene (LT) biosynthesis inhibitor to determine whether this type of inhibitor (such as 5) interacts with a novel protein, critical for LT biosynthesis. One of the key transformations was to introduce a tritium label in the thiazole ring. This was eventually achieved by treating the iodinated compound with tritium, Pt/C (sulfided) and triethylamine in anhydrous aprotic solvent, to give the tritiated compound with a specific activity of 303 GBq/mmol. The affinity probe will be used to identify the proteins and protein complexes with which this type of molecules interacts with in inflammatory cells. Copyright © 2010 John Wiley & Sons, Ltd.