N,N-Diacetyl-O-methylhydroxylamine → HCID 74020018、化合物

反応式

[NH2:1][CH2:2][CH2:3][O:4][N:5]=[CH:6][C:7]1[C:8]([F:30])=[C:9]([F:29])[C:10]([NH:20][C:21]2[CH:26]=[CH:25][C:24]([I:27])=[CH:23][C:22]=2[F:28])=[C:11]([CH:19]=1)[C:12]([NH:14][O:15][CH2:16][CH2:17][OH:18])=[O:13].CON(C(C)=O)[C:34](=[O:36])[CH3:35]>CN(C)C=O.CO>[C:34]([NH:1][CH2:2][CH2:3][O:4][N:5]=[CH:6][C:7]1[C:8]([F:30])=[C:9]([F:29])[C:10]([NH:20][C:21]2[CH:26]=[CH:25][C:24]([I:27])=[CH:23][C:22]=2[F:28])=[C:11]([CH:19]=1)[C:12]([NH:14][O:15][CH2:16][CH2:17][OH:18])=[O:13])(=[O:36])[CH3:35]

参加物

実験手順

To a solution of 5-[(2-amino-ethoxyimino)-methyl]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-benzamide (8.14 mg, 0.02 mmol) described in Example 22 in a mixture of dimethylformamide (1 ml) and methanol (5 ml), N-methoxy-diacetamide (100 mg, 0.76 mmol) was added, and the mixture was stirred at room temperature for 14 hours. After completion of the reaction, the solvent was distilled off under reduced pressure, and the resulting residue was purified with Mega Bond Elut silica gel (5 g, Varian, Inc.). From the fractions eluted with 6% methanol/methylene chloride, 5-[(2-acetylamino-ethoxyimino)-methyl]-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-benzamide (8.10 mg, 92% yield) was obtained as a pale yellow solid.