Bis(tributyltin) oxide → 4-(2-Fluoro-4-iodo-phenylamino)-1-(toluene-4-sulfonyl)-1H-indazole-5-carboxylic acid
反応式
C[O:2][C:3]([C:5]1[C:6]([NH:24][C:25]2[CH:30]=[CH:29][C:28]([I:31])=[CH:27][C:26]=2[F:32])=[C:7]2[C:11](=[CH:12][CH:13]=1)[N:10]([S:14]([C:17]1[CH:22]=[CH:21][C:20]([CH3:23])=[CH:19][CH:18]=1)(=[O:16])=[O:15])[N:9]=[CH:8]2)=[O:4].CCCC[Sn](O[Sn](CCCC)(CCCC)CCCC)(CCCC)CCCC>C1(C)C=CC=CC=1>[F:32][C:26]1[CH:27]=[C:28]([I:31])[CH:29]=[CH:30][C:25]=1[NH:24][C:6]1[C:5]([C:3]([OH:4])=[O:2])=[CH:13][CH:12]=[C:11]2[C:7]=1[CH:8]=[N:9][N:10]2[S:14]([C:17]1[CH:18]=[CH:19][C:20]([CH3:23])=[CH:21][CH:22]=1)(=[O:16])=[O:15]参加物
4
実験手順
To a solution of 4-(2-fluoro-4-iodophenylamino)-1-(toluene-4-sulfonyl)-1H-indazole-5-carboxylic acid methyl ester (0.51 g, 0.91 mmol) in toluene (5 mL) was added bis(tributyltin) oxide (0.92 mL, 1.8 mmol) and the reaction mixture heated at reflux for 48 hours. The reaction mixture was concentrated in vacuo and the resultant residue subjected to flash chromatography (Si—PPC, gradient 0-10% methanol in DCM) to yield the title compound as a light brown solid (0.46 g, 92%). LCMS (Method B): RT=4.27 min, [M+H]+=552.