反应详情

温度

95 °C

2-Bromo-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((S)-2-methoxy-1-methyl-ethyl)-amide (100 mg, 0.196 mmol) and hexamethyltin (72 mg, 0.22 mmol) were combined in a nitrogen sparged toluene (5 ml) solution. Tetrakis(triphenylphosphine)palladium(0) (19.5 mg, 0.17 mmol) was added and the solution heated to 95° C. for 2 h. The reaction was cooled and 3-iodo-imidazo[1,2-a]pyridine-7-carbonitrile (54 mg, 0.2 mmol) was added with additional tetrakis(triphenylphosphine)palladium(0) (20 mg, 0.02 mmol). The mixture was heated at 100° C. for 14 h, cooled and directly purified by silica gel chromatography to afford 2-(7-cyano-imidazo[1,2-a]pyridin-3-yl)-5-(2-trimethylsilanyl-ethoxymethyl)-5H-pyrrolo[2,3-b]pyrazine-7-carboxylic acid ((S)-2-methoxy-1-methyl-ethyl)-amide.

1. customsparged toluene (5 ml) solution
2. temperatureThe reaction was cooled
3. temperatureThe mixture was heated at 100° C. for 14 h
4. temperaturecooled
5. customdirectly purified by silica gel chromatography