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With caesium carbonate;tetrakis(triphenylphosphine) palladium(0); In 1,4-dioxane; water; at 75℃; for 4h;
Preparation 1Methyl 3,5-diamino-6-r2-(trifluoromethoxy)phenyllpyrazine-2-carboxylateMETHOD AMethyl 3,5-diamino-6-chloropyrazine~2-carboxylate (1.62 g, 8.0 mmol) was combined with 2-(trifluoromethyl)phenylboronic acid (3.29 g: 16.0 mmol), palladium tetrakistriphenylphosphine (0.924 g, 0.80 mmol) and cesium carbonate (2.61 g, 8.0 mmol) and suspended in a mixture of 1 ,4-dioxane (30 ml) and water (15 ml). The reaction was sealed and heated to 750C for 4 hours before cooling to room temperature. Water (150 ml) was added and the 1 ,4-dioxane removed in vacuo. The precipitate formed was collected by filtration and dried. The brown solid was triturated with dichloromethane:methanol, then purified by silica gel column chromatography eluting with 95:5 dichloromethane:methanol to afford the title compound as a yellow solid (1.66 g, 63percent yield).1HNMR (d6-DMSO): 3.7 (s, 3H), 6.59 (br s, 2H), 7.10 (br s, 2H), 7.41-7.64 (m, 4H) LCMS Rt=8.64 min MS m/z 329 [MH]+
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