HCID 16776699, compound → HCID 86624172, compound

Participants

Reaction Steps

Use a method similar to the General Procedure 1-3 to couple 7-chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethanesulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine (0.33 g, 0.78 mmol) with a solution of 4-(2,2-dimethyl-propionylamino)-benzylamine (0.32 g, 1.6 mmol) in anhydrous toluene/dioxane (4:1, 10 mL). Purify the crude mixture by chromatography on silica gel eluting with hexane/EtOAc (1:0 to 7:3 gradient over 30 min; 35 mL/min) and then by SCX chromatography to obtain 7-chloro-6-[4-(2,2-dimethyl-propionylamino)-benzylamino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine as a yellow oil (0.266 g, 70%). MS (ES+) m/z: 482 (M+H)+.

Provenance & Evidence