Cesium fluoride → HCID 59003117, compound

Participants

Reaction Steps

Combine tert-butyl-5-[acetyl-(3,5-bistrifluoromethylbenzyl)amino]-8-bromo-2,3,4,5-tetrahydrobenzo[b]azepine-1-carboxylate (0.438 g, 0.719 mmol), methylboronic acid (0.086 g, 1.44 mmol), [1,1′-bis(diphenylphosphino)ferrocene]dichloropalladium(II), complex with dichloromethane (1:1) (0.059 g, 0.072 mmol) and cesium fluoride (0.328 g, 2.16 mmol) in dioxane (2.5 mL) in a 10 mL microwave vessel and irradiate this mixture at 110° C. for 80 min. Dilute the cooled mixture with dichloromethane and filter through Celite®. Remove the filtrate solvent under reduced pressure and purify the residue first using chromatography on silica gel, eluting with hexanes/ethyl acetate (60:40), to afford the title compound as a white solid (0.116 g, 30%).

Provenance & Evidence