Diisopropylethylamine → 2-{4-[(R)-3-Hydroxy-1-(6-methyl-pyridin-3-yl)-propylamino]-7,8-dihydro-5H-pyrido[4,3-d]pyrimidin-6-yl}-5-methyl-benzonitrile

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A reaction mixture of 2-(4-chloro-7,8-dihydropyrido[4,3-d]pyrimidin-6(5H)-yl)-5-methylbenzonitrile (60 mg, 0.21 mmol) and (R)-3-amino-3-(6-methylpyridin-3-yl)propan-1-ol (35 mg, 0.21 mmol) in acetonitrile (2 mL) and N,N-diisopropylethylamine (73 μL, 0.42 mmol) was subjected to microwave irradiation at 180° C. for 3 h. The reaction mixture was concentrated and the residue was purified by silica gel column (0-30% MeOH/CH2Cl2) followed by preparative HPLC (100×20.2 mm, C18 column; 20-50% CH3CN-water [10 mM Et2NH]) to yield an off-white solid (29 mg).

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