7-Chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethylsulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine → HCID 86624166, compound

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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 (705 mg, 1.66 mmol) and 2-aminomethyl-5-cyclohexyloxy-pyridine (410 mg, 1.99 mmol). Purify the crude mixture by chromatography on silica gel (150 g, pre-packed cartridge) eluting with hexane/EtOAc (1:0 to 9:1 gradient) to obtain 7-chloro-6-[(5-cyclohexyloxy-pyridin-2-ylmethyl)-amino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (520 mg, 65%). MS (APCI+) m/z: 482 (M+H)+.

Provenance & Evidence