Ethanol → HCID 118113476, compound

Participants

Reaction Conditions

Reaction Steps

Carbon monoxide at 10 atm was introduced to a mixture of 1.07 g of 5-chloro-3-ethylsulfonyl-N-methyl-N-(4-trifluoromethylsulfanylphenyl)picolinamide (Compound of Present Invention 118), 6 mg of palladium(II) acetate, 80 mg of 1,1′-bis(diphenylphosphino)ferrocene, 410 mg of sodium acetate and 20 ml of ethanol, and the mixture was stirred at 110° C. for 3 hours. 6 mg of palladium(II) acetate and 80 mg of 1,1′-bis(diphenylphosphino)ferrocene were added to the cooled reaction mixture, then carbon monoxide at 10 atm was introduced, and the mixture was stirred at 130° C. for 3 hours. The cooled reaction mixture was poured to water, and the mixture was extracted with ethyl acetate. The organic layer was dried over anhydrous sodium sulfate and then concentrated under reduced pressure, and the resulting residue was applied to a silica gel column chromatography to obtain 0.96 g of ethyl 5-ethylsulfonyl-6-[methyl-(4-trifluoromethylsulfanylphenyl) carbamoyl]nicotinate (hereinafter, referred to as Compound of Present Invention 125).

Provenance & Evidence