7-Chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethylsulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine → HCID 86624163, 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 (245 mg, 0.58 mmol) with 2-aminomethyl-5-cyclopentylthiomethyl-pyridine (230 mg, 1 mmol) in toluene (5 mL). Purify the crude mixture by chromatography on silica gel eluting with hexane/THF (49:1 to 7:3 gradient) to obtain 7-chloro-6-[(5-cyclopentylthiomethyl-pyridin-2-ylmethyl)-amino]-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine (170 mg, 59%). MS (ES+) m/z: 498.1 (M+H)+.

Provenance & Evidence