Water → [7-(3-Methanesulfonyl-pyridin-2-yl)-5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidin-4-yl]-(4-trifluoromethyl-phenyl)-amine

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Reaction Conditions

Reaction Steps

N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-amine prepared as described in Example 1.D. (0.100 g, 0.34 mmol) was dissolved in a mixture of dioxane/N,N-dimethylacetamide (10:1) (1.1 mL). To the solution was added 2-chloro-3-(methylsulfonyl)pyridine (Ponticello et al, J. Org. Chem., 44(17), 1979) (0.128 mg, 0.67 mmol) and N,N-diisopropylethylamine (0.09 mL, 0.51 mmol). The mixture was heated via microwave (Emrys Optimizer model, Personal Chemistry) at 150° C. for 20 min. The reaction mixture was poured into water (20 mL) and extracted with ethyl acetate (2×20 mL). The combined organic layers were washed with brine, dried over magnesium sulfate, and concentrated to leave a solid. The solid was purified by silica gel chromatography using a gradient of ethyl acetate:hexane (0-100%) to give the desired compound as an white solid (75 mg, 49%).

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