反应详情

Use a method similar to the General Procedure 5-3 to couple 7-chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethanesulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine (0.3 g, 0.706 mmol) with 3-phenyl-benzylamine (0.388 g, 2.117 mmol) using palladium(II) acetate (32 mg, 0.141 mmol), tris(dibenzylideneacetone)dipalladium(0) (65 mg, 0.070 mmol), BINAP (264 mg, 0.424 mmol) and cesium carbonate (460 mg, 1.412 mmol) in toluene (12 mL). Purify by chromatography on silica gel eluting with hexane/EtOAc (1:0, 19:1) to give 7-chloro-6-(3-phenyl-benzylamino)-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine as an oil (0.257 g, 79%). MS (ES+) m/z: 459 (M+H)+.

1. customPurify by chromatography on silica gel eluting with hexane/EtOAc (1:0, 19:1)