Toluene → HCID 68579342, compound

Participants

Reaction Steps

A solution of tert-butyl 6-bromo-2,3-dihydro-1,4-benzoxazepine-4(5H)-carboxylate (500 mg, 1.52 mmol), (3S)-3-methylmorpholine p-toluenesulfonate (416 mg, 1.52 mmol), 2-dicyclohexylphosphino-2′,4′,6′-triisopropylbiphenyl(X-phos) (58.0 mg, 0.122 mmol), tris(dibenzylideneacetone)dipalladium(0) (27.8 mg, 0.0304 mmol), sodium tert-butoxide (365 mg, 3.80 mmol) and toluene (6 ml) was stirred under an argon atmosphere at 100° C. for 12 hr. The reaction mixture was poured into water, and the mixture was extracted with ethyl acetate. The extract was washed with water and dried over anhydrous magnesium sulfate. The solvent was evaporated under reduced pressure. The residue was purified by silica gel column chromatography (hexane:ethyl acetate=1:1) to give the desired product (420 mg, 79.2%) as an oil.

Provenance & Evidence