1,4-Dibromobutane → 2-{[(1S,2S)-2-pyrrolidin-1-ylcyclohexyl]amino}-6-(trifluoromethyl)nicotinic acid

Participants

Reaction Conditions

Reaction Steps

Diisopropylethylamine and (1S,2S)-1,2-cyclohexandiamine were added to 2-chloro-6-(trifluoromethyl)nicotinic acid, followed by stirring at 100° C. for 30 minutes and at 140° C. for 10 minutes using a microwave reaction device. The reaction liquid was dissolved in acetonitrile, potassium carbonate and 1,4-dibromobutane were added, followed by stirring at 50° C. for 8 hours. By dissolving the residue extracted with chloroform in methanol and THF, adding 1 M sodium hydroxide aqueous solution thereto and carrying out the reaction at 50° C., 2-{[(1S,2S)-2-pyrrolidin-1-ylcyclohexyl]amino}-6-(trifluoromethyl)nicotinic acid was obtained.

Provenance & Evidence