反应详情

A solution of 1-(6-methylpyrimidin-4-yl)piperidin-4-amine (52.5 mg, 273 μmol), tert-butyl 3-(2-bromo-6-methyl-[1,2,4]triazolo[1,5-a]pyridin-8-yl)benzylcarbamate (114 mg, 273 mmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (12.6 mg, 21.9 μmol), tris(dibenzylideneacetone)dipalladium(0) chloroform adduct (11.3 mg, 10.9 μmol) and sodium phenoxide (50.1 mg, 410 μmol) in dioxane (3 mL) was degassed three times and reacted at 140° C. under an atmosphere of nitrogen in a microwave oven for 1 hour. The title compound was obtained a light yellow solid (46 mg, 32%) after column chromatography on silica gel using a gradient from methylenechloride to a mixture of methylenechlorid/methanol 19:1 (v/v) as eluent.

1. customreacted at 140° C. under an atmosphere of nitrogen in a microwave oven for 1 hour