Preparation of a Series of 5-Methyl-3-(substituted)-[1,2,4]triazines. 2011

Moses G Gichinga, and Jeremy P Olson, and Elizabeth Butala, and Brian P Gilmour, and Hernán H Navarro, and F Ivy Carroll
Center for Organic and Medicinal Chemistry, Research Triangle Institute, P.O. Box 12194, Research Triangle Park, North Carolina 27709.

Procedures for the synthesis of thirty-six 5-methyl-3-(substituted)-[1,2,4]triazines have been described. These compounds were evaluated for antagonism at metabotropic glutamate receptor subtype 5. Two compounds, 5b and 3c, were determined to be low micromolar inhibitors of mGluR5.

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