Cesium carbonate → HCID 86624192, compound

Participants

Reaction Steps

Use a method similar to the General Procedure 1-2 to couple 7-chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethanesulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine (173 mg, 0.4 mmol) with 4-[2-(2,2,2-trifluoroethylthio)-1,1-(ethylenedioxy)ethyl]-benzylamine (250 mg, 0.8 mmol) using tris(dibenzylideneacetone)dipalladium(0) (73.2 mg, 0.08 mmol), BINAP (106 mg, 0.16 mmol) and cesium carbonate (182 mg, 0.6 mmol) in toluene (20 mL). Purify by chromatography on silica gel eluting with hexane/EtOAc (75:25) to give 7-chloro-3-(2,2,2-trifluoroacetyl)-6-{4-[2-(2,2,2-trifluoroethylthio)-1,1-(ethylenedioxy)ethyl]-benzylamino}-2,3,4,5-tetrahydro-1H-benzo[d]azepine (97 mg, 41%).

Provenance & Evidence