反应详情

N-[2-Chloro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-benzenesulfonamide (Intermediate B) (50 mg, 0.13 mmol), 5-Bromo-4-methyl-pyrimidin-2-ylamine (Intermediate C) (26 mg, 0.14 mmol) and PdCl2(dppf).DCM (10 mg, 0.013 mmol) are placed in a microwave vial containing degassed DME (3 ml) and 2M Na2CO3 (1 ml). The resulting mixture is heated using microwave radiation at 100° C. for 45 minutes. The reaction mixture is diluted with DCM, MgSO4 is added and the mixture is filtered through Celite® (filter agent). The filtrate is absorbed onto silica and purification by flash chromatography on silica eluting with MeOH:DCM (1% to 2% MeOH) affords the title compound.

1. additioncontaining
2. customdegassed DME (3 ml) and 2M Na2CO3 (1 ml)
3. temperatureThe resulting mixture is heated
4. customat 100° C.
5. customfor 45 minutes
6. additionThe reaction mixture is diluted with DCM, MgSO4
7. additionis added
8. filtrationthe mixture is filtered through Celite® (filter agent)
9. customThe filtrate is absorbed onto silica and purification by flash chromatography on silica eluting with MeOH