反应详情

温度

85 °C

A mixture of 5,8-dibromoimidazo[1,2-a]pyrazine (1.0 g, 3.6 mmol), 4-amino-N-(2-diethylaminoethyl)benzenesulfonamide (109 mg, 0.4 mmol), Pd2(dba)3 (7 mg, 0.007 mmol), Xantphos (8.4 mg, 0.015 mmol) and Cs2CO3 (167 mg, 0.52 mmol) in dioxane is heated at 85° C. under nitrogen for 18 hours. The reaction is cooled to room temperature then evaporated to dryness. The residue is chromatographed on silica gel, eluting with DCM then 98:2 DCM:NH3 (7N in MeOH), and the fractions containing the title compound are combined and evaporated to afford a dark oil. This oil contains an impurity, but is used in the subsequent step without further purification.

1. temperatureThe reaction is cooled to room temperature
2. customthen evaporated to dryness
3. customThe residue is chromatographed on silica gel
4. washeluting with DCM
5. addition98:2 DCM:NH3 (7N in MeOH), and the fractions containing the title compound
6. customevaporated
7. customto afford a dark oil
8. customis used in the subsequent step without further purification