تفاعل #53706

معادلة التفاعل

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

trans-2-(4-fluorophenyl)vinylboronic acid

sodium hydrogencarbonate

→

N-{3-[(E)-2-(4-fluorophenyl)vinyl]-1H-indazol-5-yl}-2-methylsulfonylbenzenesulfonamide

المردود 29.4%

المذيبات

dimethylformamide

ظروف التفاعل

الإجراء التجريبي

N-{3-[(E)-2-(4-Fluorophenyl)vinyl]-1H-indazol-5-yl}-2-methylsulfonylbenzenesulfonamide can be obtained as described in Example 59 from 1 g of tert-butyl 3-iodo-5-(2-methylsulfonylbenzenesulfonylamino)-indazole-1-carboxylate, 575 mg trans-2-(4-fluorophenyl)vinylboronic acid, 28 ml of dimethylformamide, 3.25 ml of a saturated aqueous sodium hydrogencarbonate solution and 41 mg of tetrakis(triphenylphosphine)palladium[0]. 240 mg of N-{3-[(E)-2-(4-fluorophenyl)vinyl]-1H-indazol-5-yl}-2-methylsulfonylbenzenesulfonamide are thus obtained in the form of an off-white solid melting at 248° C. (analysis C22H18FN3O4S2 % calculated C, 56.04; H, 3.85; F, 4.03; N, 8.91; O, 13.57; S, 13.60. % found C, 56.21; H, 4.09; F, 3.95; N, 8.64; S, 13.31).

المصدر