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Synthesis 2012(1): 57-62  
DOI: 10.1055/s-0031-1289587
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

A Practical, Laboratory-Scale Synthesis of Perampanel

Charles J. McElhinny Jr., F. I. Carroll, Anita H. Lewin*
Research Triangle Institute, 3040 Cornwallis Road, Research Triangle Park, NC 27709, USA
Fax: +1(919)5418868; e-Mail: ahl@rti.org;
Further Information

Publication History

Received 27 September 2011
Publication Date:
04 November 2011 (online)

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Abstract

The orally active, noncompetitive, selective AMPA receptor antagonist Perampanel, 2-[1′,6′-dihydro-6′-oxo-1-phenyl-(2′,3′-bipyridin)-5′-yl]benzonitrile, has been prepared from readily available, relatively inexpensive starting materials. The synthesis was carried out on a laboratory scale with no specialized equipment, and involved only two chromatographic purifications.

Key words

AMPA antagonist - Suzuki coupling - palladium content - Stille coupling - trace-metal contamination

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