反应详情

温度

110 °C

To an argon purged solution of 4-(7-bromo-[1,2,4]triazolo[1,5-a]pyridin-2-yl)morpholine (321 mg, 1.13 mmol) in dioxane (8 ml) are added tert-butyl carbamate (159 mg, 1.36 mmol), tris(dibenzylideneacetone)dipalladium(0) (20.8 mg, 22.7 μmol), 4,5-bis(diphenylphosphino)-9,9-dimethylxanthene (26.2 mg, 45.4 μmol) and cesium carbonate (517 mg, 1.59 mmol). The reaction vessel is sealed and heated to 110° C. for 20 hours. The crude material is applied on silica and purified by flash chromatography on a 20 g silica column using heptane/ethyl acetate 10-70% as eluent affording tert-butyl 2-morpholino-[1,2,4]triazolo[1,5-a]pyridin-7-ylcarbamate (365 mg, 101%) as a light yellow solid. mp.: 92-3° C. MS: m/z=320.1 (M+H+).

1. customThe reaction vessel is sealed
2. custompurified by flash chromatography on a 20 g silica column