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[ 14 C]Dimethyltitanocene and [ 14 C]Methyl(methyltrimethylsilyl) titanocene–Reagents for the [ 14 C]olefination of carbonyl compounds: synthesis of [ 14 C]Aprepitant
Author(s) -
Wallace M. A.,
Dean D. C.,
Melillo D. G.
Publication year - 2009
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.1667
Subject(s) - aprepitant , chemistry , reagent , methyllithium , antagonist , stereochemistry , combinatorial chemistry , organic chemistry , receptor , biochemistry , medicine , surgery , antiemetic , vomiting
A neurokinin (NK‐1) receptor antagonist, [ 14 C]Aprepitant, was synthesized using two labeled olefination reagents: [ 14 C]dimethyltitanocene 1 and [ 14 C]methyl (methyltrimethylsilyl)titanocene 7. Both reagents can be readily prepared from [ 14 C]methyllithium and have been shown to convert a variety of carbonyls to [ 14 C]methylenes in good radiochemical yields. Copyright © 2009 John Wiley & Sons, Ltd.