Methanol → 3-{[6-(3-Methanesulfonyl-phenyl)-4-(2,2,2-trifluoro-ethylamino)-pyrido[3,2-d]pyrimidin-2-ylamino]-methyl}-benzenesulfonamide

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Reaction Steps

(2,6-Dichloro-pyrido[3,2-d]pyrimidin-4-yl)-(2,2,2-trifluoro-ethyl)-amine (2.3 g) and 3-Aminomethyl-benzenesulfonamide (0.336 g) were dissolved in NMP (10 mL) and dioxane (10 mL), treated with diisopropylethylamine (0.160 mL) and heated to reflux. After 8 h, additional portions of 3-Aminomethyl-benzenesulfonamide (440 mg) and diisopropylethylamine (0.200 mL). After an additional 12 h of heating, additional diisopropylethylamine was added (1.2 mL). The reaction mixture was stirred for another 24 h at reflux. Methanol (30 mL) was added followed by water (80 mL) and the mixture was allowed to cool to ambient temperature. A precipitate was collected and washed with 10% MeOH:water, and dried to give 1.2 g of the desired product which was used without further purification.

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