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Synthesis of 14C-labeled and tritiated AMPA potentiator LY450108

✍ Scribed by Boris A. Czeskis; Douglas D. O'Bannon; William J. Wheeler; Dean K. Clodfelter

Publisher: John Wiley and Sons
Year: 2005
Tongue: French
Weight: 165 KB
Volume: 48
Category: Article
ISSN: 0022-2135
DOI: 10.1002/jlcr.899

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✦ Synopsis

Asymmetric synthesis of AMPA potentiator LY450108-[ 14 C] containing 14 C-label attached to the chiral center of the molecule, was accomplished based on Evans' chiral oxazolidinone auxiliary method. Diastereoselective methylation of p-nitrophenylacetic acid derivative was used as a key step. The auxiliary was reductively removed, and the resulting primary alcohol was converted into the corresponding amine. Its sulfonylation, reduction of the aromatic nitro group, and acylation with 3,5difluorobenzoyl chloride led to the final product. The synthesis of tritiated LY450108 is also detailed.

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