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

Jeremy P. Olson; F. Ivy Carroll

doi:10.1055/s-0030-1258376

PAPER

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;

Abstract

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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

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References

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