The synthesis of k -l a b e l l e d methyl benzyl n i t r o s - amine is reported. Two fonns were prepared, one with a l a b e l i n the methyl group and one with l a b e l i n the methylene portion of t h e benzyl group. a c t i v i t i e s were approximately 5 mCi/mmol.
[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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