5-Bromosalicylic acid → HCID 68547977, compound

Participants

Reaction Steps

A mixture of 5-bromosalicylic acid (326 mg, 1.5 mmol), [1-(4-amino-2-fluorophenyl)piperidin-4-yl]carbamic acid tert-butyl ester (compound of Reference Example 90; 309 mg, 1.0 mmol), 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide hydrochloride (287 mg, 1.5 mmol), 1-hydroxybenzotriazole (202 mg, 1.5 mmol), triethylamine (210% 1, 1.5 mmol) and N,N-dimethylformamide (5 ml) was stirred at room temperature for 3 hours. Saturated aqueous sodium hydrogen carbonate and water was added to the reaction mixture and the mixture was carried out ultrasound irradiation. The precipitated solid was collected by filtration and washed with water. The solid was suspended in methanol and carried out ultrasound irradiation. The solid was collected by filtration and dried under reduced pressure to give the title compound (224 mg, 47%) as a white solid.

Provenance & Evidence