反应详情

A mixture of 4-bromo-1,2-dimethyl-3-(1-methylindolin-6-yl)-1H-pyrrolo[2,3-b]pyridine (D28) (390 mg, 1.095 mmol), 1-methyl-1H-pyrazole-3-sulfonamide (D94) (265 mg, 1.642 mmol), (9,9-dimethyl-9H-xanthene-4,5-diyl)bis(diphenylphosphine) (95 mg, 0.164 mmol), cesium carbonate (1070 mg, 3.28 mmol) and Pd2(dba)3 (75 mg, 0.082 mmol) in 1,4-dioxane (10 mL) was refluxed for 7 hours. After cooled to RT, the reaction mixture was filtered through celite, washing with DCM and the resulting solution was evaporated to dryness. DCM was added to the residue and the resulting solid was filtered and then taken up in formic acid/DMSO (1:1), purified by MDAP (acidic condition) to give the title compound (155 mg). LCMS (A): m/z (M+H)+ 437, C22H24N6O2S requires 436 (acidic).

1. temperaturewas refluxed for 7 hours
2. filtrationthe reaction mixture was filtered through celite
3. washwashing with DCM
4. customthe resulting solution was evaporated to dryness
5. additionDCM was added to the residue
6. filtrationthe resulting solid was filtered
7. custompurified by MDAP (acidic condition)