Triethylamine → HCID 66680346, compound

Participants

Reaction Steps

A catalytic amount of DMF and 114 mg (0.900 mmol) of oxalyl chloride were added at 0° C. to 2 mL of THF solution comprising 119 mg (0.600 mmol) of biphenyl-3-carboxylic acid, and the mixture was stirred at room temperature for 40 minutes. The solvent was distilled off under reduced pressure, and then 2 mL of DMAc, 200 mg (0.600 mmol) of the methyl 5-chloro-2-[(piperidin-3-ylcarbonyl)amino]benzoate hydrochloride obtained in Example 11-(ii), and 0.092 mL (0.660 mmol) of triethylamine were added in this order to the residue at 0° C., and the mixture was stirred for 3 hours. After the completion of the reaction, saturated sodium bicarbonate water was added under ice-cooling, and the mixture was stirred. The resulting solids were collected by filtration, washed with water, and dried under reduced pressure at 50° C. for 3 hours, thereby giving 270 mg of methyl 2-({[1-(biphenyl-3-ylcarbonyl)piperidin-3-yl]carbonyl}amino)-5-chlorobenzoate (yield: 94%).

Provenance & Evidence