Sodium Carbonate → HCID 86622787, compound

Participants

Reaction Conditions

Reaction Steps

Dissolve 7-chloro-3-(2,2,2-trifluoroacetyl)-6-trifluoromethanesulfonyloxy-2,3,4,5-tetrahydro-1H-benzo[d]azepine (425 mg, 1 mmol), bis(triphenylphosphine)-palladium(II) chloride (0.1 equiv.), 4-[(cyclopentanecarbonyl-amino)-methyl]-phenyl-boronic acid (490 mg, 2.0 mmol) and sodium carbonate (2 equiv.) in THF/water (2:1, 15 mL) and heat the mixture at 80° C. for 6 h. Cool the reaction mixture to ambient temperature, dilute with EtOAc and wash with water. Dry the organic fraction over MgSO4, filter and concentrate in vacuo to obtain 7-chloro-6-{4-[(cyclopentanecarbonyl-amino)-methyl]-phenyl}-3-(2,2,2-trifluoroacetyl)-2,3,4,5-tetrahydro-1H-benzo[d]azepine, suitable for use without further purification.

Provenance & Evidence