反应详情

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 (400 mg, 0.94 mmol) with 4-(morpholin-4-ylmethyl)-benzylamine (291 mg, 1.41 mmol). Purify by chromatography on silica gel (80 g, pre-packed cartridge) eluting with hexane/EtOAc (1:0 to 2:1 gradient) to obtain 7-chloro-6-[4-(morpholin-4-ylmethyl)-benzylamino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (304 mg, 67%). MS (APCI+) m/z: 482 (M+H)÷.

1. customPurify by chromatography on silica gel (80 g, pre-packed cartridge)
2. washeluting with hexane/EtOAc (1:0 to 2:1 gradient)