反应详情

To a 0.5 M solution of 2-bromo-2-(5-fluoropyridin-2-yl)acetic acid in 99:1 DCM/DMF is added oxalyl chloride (1.2 equiv) and the mixture is allowed to stir at rt for 30 min or until the reaction is substantially complete. The mixture is then cooled to 0° C. and 2-aminobenzamide (1 equiv) in pyridine (2 mL) is added slowly, and the mixture is allowed to warm to rt over ca. 1 h. The mixture is concentrated under reduced pressure and the residue is purified by chromatography to afford 2-(2-bromo-2-(5-fluoropyridin-2-yl)acetamido)benzamide.

1. temperatureThe mixture is then cooled to 0° C.
2. temperatureto warm to rt over ca. 1 h
3. concentrationThe mixture is concentrated under reduced pressure
4. customthe residue is purified by chromatography