Reacción #53693

Ecuación de reacción

tert-butyl 3-iodo-5-(N-tert-butoxycarbonyl-2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate

1-(tert-butoxycarbonyl)-7-azaindole-2-boronic acid

sodium hydrogencarbonate

→

2-methylsulfonyl-N-[3-(1H-pyrrolo[2,3-b]pyridin-2-yl)-1H-indazol-5-yl]benzenesulfonamide

Rendimiento 45.9%

Disolventes

dimethylformamide

Condiciones de reacción

Procedimiento

2-Methylsulfonyl-N-[3-(1H-pyrrolo[2,3-b]pyridin-2-yl)-1H-indazol-5-yl]benzenesulfonamide can be obtained as described in Example 47 from 157.7 mg of tert-butyl 3-iodo-5-(N-tert-butoxycarbonyl-2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate, 122 mg of 1-(tert-butoxycarbonyl)-7-azaindole-2-boronic acid, 7 ml of dimethylformamide, 500 μl of a saturated aqueous sodium hydrogencarbonate solution and 6.7 mg of tetrakis(triphenylphosphine)palladium[0]. 50 mg of 2-methylsulfonyl-N-[3-(1H-pyrrolo[2,3-b]pyridin-2-yl)-1H-indazol-5-yl]benzenesulfonamide are thus obtained in the form of a creamy yellow solid which decomposes at approximately 200° C. (LC/MS analysis: Tr 2.88 minutes MH+=468).

Fuente