反应详情

温度

-78 °C

BBr3 (2.81 mL, 1.0M in DCM, 2.81 mmol) is added to a suspension of 3-{[3-(4-Methoxy-phenyl)-imidazo[1,2-a]pyrazin-8-ylamino]-methyl}-benzenesulfonamide (0.115 g, 0.281 mmol) in DCM (3 mL) at −78° C. under nitrogen atmosphere. The reaction is allowed to warm to r.t and monitored by analytical HPLC. After 2 h the reaction is complete and is cooled to −78° C., quenched with a solution of saturated aqueous K2CO3. The reaction is diluted with AcOEt, washed with water, dried with MgSO4 anh., filtered and evaporated to give 0.058 g of 3-{[3-(4-Hydroxy-phenyl)-imidazo[1,2-a]pyrazin-8-ylamino]-methyl}-benzenesulfonamide as a brown oil (52%). No further purification was required. LC-MS m/z 396 [M+H]+.

1. temperatureto warm to r.t and
2. customquenched with a solution of saturated aqueous K2CO3
3. additionThe reaction is diluted with AcOEt
4. washwashed with water
5. dry with materialdried with MgSO4 anh.
6. filtrationfiltered
7. customevaporated