HCID 28755594, compound → HCID 86624174, 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 (0.23 g, 0.53 mmol) with a solution of 4-(N-methyl-2,2-dimethyl-propionylamino)-benzylamine (0.23 g, 1.06 mmol) in anhydrous toluene/dioxane (4:1, 7 mL). Purify by chromatography on silica gel eluting with hexane/EtOAc (1:0 to 17:3 gradient over 30 min, 17:3 over 30 min, 17:3 to 7:3 gradient over 30 min and 7:3 over 30 min; 35 mL/min) to obtain 7-chloro-6-[4-(N-methyl-2,2-dimethyl-propionylamino)-benzylamino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]-azepine as a yellow oil (0.235 g, 90%).

Provenance & Evidence