反应详情

The crude 2-chloro-N-(4-hydroxy-cyclohexyl)-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzenesulfonamide from step 2 (1.48 g), 5-Bromo-4 methyl-pyrimidin-2-ylamine (intermediate C) (0.669 g, 3.36 mmol) and PdCl2(dppf).DCM (0.436 g, 0.53 mmol) are placed in a microwave vial containing degassed DME (10 ml) and 2M Na2CO3 (2 ml). The resulting mixture is heated using microwave radiation at 100° C. for 15 minutes. After evaporation of the solvent, the reaction mixture is purified by flash chromatography on silica eluting with ethanol to afford the title compound.

1. additioncontaining
2. customdegassed DME (10 ml) and 2M Na2CO3 (2 ml)
3. temperatureThe resulting mixture is heated
4. customat 100° C.
5. customfor 15 minutes
6. customAfter evaporation of the solvent
7. customthe reaction mixture is purified by flash chromatography on silica eluting with ethanol