Boron tribromide → HCID 86723792, compound

Participants

Reaction Conditions

Reaction Steps

To a 0° C. solution of 6-chloro-4-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-methoxy-3,4-dihydro-1,4-benzoxazepin-5(2H)-one (124c, 500 mg, 1.38 mmol) in anhydrous DCM (10 mL) was added slowly a solution of BBr3 (1 M in DCM, 4.00 mL, 4.00 mmol). The reaction mixture was stirred at 0° C. for 3 hours, then quenched with water, and further diluted with water to 100 mL. The resulting mixture was extracted with DCM (3×100 mL). The combined organic phases were dried over sodium sulfate, and concentrated under vacuum to give 6-chloro-4-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-7-hydroxy-3,4-dihydro-1,4-benzoxazepin-5(2H)-one (124d, 456 mg, 95% yield) as a solid.

Provenance & Evidence