Tetrahydrofuran → 5-{[Acetyl-(2-hydroxy-ethoxy)-amino]-methyl}-3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-benzamide

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Reaction Steps

CH3CO2H (300 mg), EDC.HCl (958 mg), and HODhbt (816 mg) were mixed in CH2Cl2 (5 mL) for 2 hours to give an active ester solution. A portion of this solution (0.2 mL) was added to a solution of 3,4-difluoro-2-(2-fluoro-4-iodo-phenylamino)-N-(2-hydroxy-ethoxy)-5-[(2-hydroxy-ethoxyamino)-methyl]-benzamide (80 mg) obtained in Example 6 and NEt3 (29 μL) in THF, and the mixture was stirred for 12 hours. The reaction mixture was washed with 0.3 N aqueous HCl and aqueous NaHCO3, and subjected to silica gel chromatography (CH2Cl2/MeOH as a developing solvent) to give the title compound (12.0 mg).

Provenance & Evidence