Morpholine → HCID 68578670, compound

Participants

Reaction Steps

A solution of tert-butyl 6-bromo-2,3-dihydro-1,4-benzoxazepine-4(5H)-carboxylate (150 mg, 0.457 mmol), morpholine (0.120 ml, 1.37 mmol), X-phos (13.0 mg, 0.0274 mmol), tris(dibenzylideneacetone)dipalladium(0) (82.4 mg, 0.00900 mmol), sodium tert-butoxide (65.8 mg, 0.684 mmol) and dioxane (3 ml) was stirred under an argon atmosphere for 2 hr at 80° C. 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=2:1) to give the desired product (120 mg, 78.4%) as an oil.

Provenance & Evidence