Ethanesulfonyl chloride → HCID 46195696, 화합물

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[NH2:1][C:2]1[CH:3]=[C:4]([CH:26]=[CH:27][CH:28]=1)[CH2:5][O:6][C:7]1[CH:15]=[C:14]([F:16])[CH:13]=[C:12]([NH:17][C:18]2[CH:23]=[CH:22][C:21]([I:24])=[CH:20][C:19]=2[F:25])[C:8]=1[C:9]([NH2:11])=[O:10].[CH2:29]([S:31](Cl)(=[O:33])=[O:32])[CH3:30]>N1C=CC=CC=1.C(OCC)(=O)C>[CH2:29]([S:31]([NH:1][C:2]1[CH:3]=[C:4]([CH:26]=[CH:27][CH:28]=1)[CH2:5][O:6][C:7]1[CH:15]=[C:14]([F:16])[CH:13]=[C:12]([NH:17][C:18]2[CH:23]=[CH:22][C:21]([I:24])=[CH:20][C:19]=2[F:25])[C:8]=1[C:9]([NH2:11])=[O:10])(=[O:33])=[O:32])[CH3:30]

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실험 절차

In analogy to GP 6b, 89 mg of 2-(3-Amino-benzyloxy)-4-fluoro-6-(2-fluoro-4-iodo-phenylamino)-benzamide (Intermediate 3.2; 0.18 mmol, 1 eq.) were dissolved in 0.75 mL pyridine, treated with 34 μL ethylsulfonyl chloride (0.36 mmol, 2 eq.). and stirred at rt for two days. the resulting mixture diluted with ethyl acetate, washed with water and the organic layers dried. Concentration in vacuo was followed by trituration to provide 84 mg of the desired compound (80% yield) with a melting point of 170° C.