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Synthesis 2011(3): 409-412  
DOI: 10.1055/s-0030-1258376
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

An Improved Synthesis of Phenylethynyl[1,2,4]methyltriazines

Jeremy P. Olson, F. Ivy Carroll*
Center for Organic and Medicinal Chemistry, Research Triangle Institute, Research Triangle Park, NC, 27709, USA
Fax: +1(919)5418868; e-Mail: fic@rti.org;
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Publication History

Received 22 September 2010
Publication Date:
20 December 2010 (online)

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Abstract

An improved synthesis of phenylethynyl[1,2,4]methyltriazines is described. In this method, 5-methyl-3-methyl­thio[1,2,4]triazine is cross-coupled with various phenylacetylenes using microwave conditions to produce phenylethynyl[1,2,4]methyltriazines in increased yields. Interest in the phenylethynyl[1,2,4]methyltriazine scaffold stems from recent reports demonstrating their potency as mGluR5 antagonists.

Key words

mGluR5 - thioether cross-coupling - triazines - microwave