反应详情

Iodomethane (91 mg, 0.64 mmoles) and potassium carbonate (88 mg, 0.64 mmoles) were added to a solution of 4-(4′-difluoromethoxy-biphenyl-4-ylaminomethyl)-5-methyl-furan-2-carboxylic acid methyl ester (170) (62 mg, 0.16 mmoles) in N,N-dimethylformamide (10 ml) and the mixture stirred at room temperature for 36 hours under an argon atmosphere. The mixture was then heated at 35° C. for 21 hours. The mixture was partitioned between dichloromethane and water, the organic phase separated and dried (MgSO4). After evaporation of the solvent, the residue was purified by flash chromatography, using cyclohexane/ethyl acetate 99:1v/v as eluent, to afford compound 175(41 mg) as a brown oil. This was used directly in part (b).

1. temperatureThe mixture was then heated at 35° C. for 21 hours
2. customThe mixture was partitioned between dichloromethane and water
3. customthe organic phase separated
4. dry with materialdried (MgSO4)
5. customAfter evaporation of the solvent
6. customthe residue was purified by flash chromatography