反应详情

N-Benzo[1,3]dioxol-5-yl-5-chloro-2-trifluoromethyl-benzenesulfonamide (0.088 g, 0.23 mmol), 4-methyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyrimidin-2-ylamine (Intermediate G, prepared according to WO 2007/084786, p. 92) (0.082 g, 0.34 mmol) and PdCl2(dppf).DCM (0.0185 g, 0.023 mmol) are placed in a microwave vial containing degassed DME (2 ml) and 2M Na2CO3 (0.23 ml). The resulting mixture is heated using microwave radiation at 120° C. for 60 minutes. After evaporation of the solvent, the reaction mixture is purified by flash chromatography on silica eluting with cyclohexane/EtOAc (1:2) to afford the title compound.

1. additioncontaining
2. customdegassed DME (2 ml) and 2M Na2CO3 (0.23 ml)
3. temperatureThe resulting mixture is heated
4. customat 120° C.
5. customfor 60 minutes
6. customAfter evaporation of the solvent
7. customthe reaction mixture is purified by flash chromatography on silica eluting with cyclohexane/EtOAc (1:2)