反应详情

A 5 ml microwave tube is charged with 5-bromo-2-chloro-N-(5-trifluoromethyl-pyridin-2-yl)-benzenesulfonamide (0.067 g, 0.16 mmol) and DME (degassed 3 ml), 4-methyl-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl]-pyrimidin-2-ylamine (Intermediate G) (0.0535 g, 0.19 mmol), 2 M aqueous Na2CO3 solution (640 μl) and PdCl2(dppf).DCM (0.00448 g, 5.4 μmol) and the mixture is heated using microwave radiation at 110° C. for 15 min. After cooling to room temperature the mixture is taken up in ethyl acetate (50 ml), washed with water, dried over MgSO4 and concentrated in vacuo. The crude product is triturated with DCM (0.5 ml), filtrated and washed with DCM to afford the pure title compound.

1. customat 110° C.
2. customfor 15 min
3. washwashed with water
4. dry with materialdried over MgSO4
5. concentrationconcentrated in vacuo
6. customThe crude product is triturated with DCM (0.5 ml)
7. filtrationfiltrated
8. washwashed with DCM