反应详情

温度

80 °C

Tert-butyl(trans-3-(2-(2-chloropyridin-3-yl)-2-methylpropanamido)cyclobutyl)carbamate (1074 mg, 2.92 mmol), sodium t-butoxide (561 mg, 5.84 mmol), and chloro(2-dicyclohexylphosphino-2′,6′-di-1-propoxy-1,1′-biphenyl)[2-(2-aminoethyl-phenyl)]palladium(ii) methyl tert-butyl ether adduct (143 mg, 0.175 mmol) were sealed in a round-bottomed flask under nitrogen. Dry dioxane (5 mL) was added and the reaction heated at 80° C. After 2 hours, the mixture was cooled and partitioned between ethyl acetate, water, and saturated ammonium chloride. The organic was dried with magnesium sulfate and evaporated to dryness to give tert-butyl(trans-3-(3,3-dimethyl-2-oxo-2,3-dihydro-1H-pyrrolo[2,3-b]pyridin-1-yl)cyclobutyl)carbamate (980 mg, 2.96 mmol, quantitative) as light-yellow solid.

1. temperaturethe mixture was cooled
2. custompartitioned between ethyl acetate, water, and saturated ammonium chloride
3. dry with materialThe organic was dried with magnesium sulfate
4. customevaporated to dryness