Reacción #53689

Ecuación de reacción

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

3-thiopheneboronic acid

sodium hydrogencarbonate

→

2-methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamide

Rendimiento 16.9%

Disolventes

dimethylformamide

Condiciones de reacción

Procedimiento

2-Methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamide can be obtained as described in Example 47 from 1 g of tert-butyl 3-iodo-5-(N-tert-butoxycarbonyl-2-methylsulfonylbenzenesulfonylamino)indazole-1-carboxylate, 376 mg of 3-thiopheneboronic acid, 40 ml of dimethylformamide, 3.2 ml of a saturated aqueous sodium hydrogencarbonate solution and 42.7 mg of tetrakis(triphenylphosphine)palladium[0]. 108 mg of 2-methylsulfonyl-N-(3-thiophen-3-yl-1H-indazol-5-yl)benzenesulfonamide are thus obtained in the form of a white solid melting at 249° C. (analysis C18H15N3O4S3 % calculated C, 49.87; H, 3.49; N, 9.69; O, 14.76; S, 22.19. % found C, 49.76; H, 3.53; N, 10.03; S, 21.78).

Fuente