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[14C]Dimethyltitanocene and [14C]Methyl(methyltrimethylsilyl) titanocene–Reagents for the [14C]olefination of carbonyl compounds: synthesis of [14C]Aprepitant

✍ Scribed by M. A. Wallace; D. C. Dean; D. G. Melillo


Publisher
John Wiley and Sons
Year
2009
Tongue
French
Weight
135 KB
Volume
52
Category
Article
ISSN
0022-2135

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✦ Synopsis


Abstract

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.


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