Cesium carbonate → HCID 86725400, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of the product of EXAMPLE 42A (280 g, 0.9 mmol), tert-butyl piperazine-1-carboxylate (205 mg, 1.09 mmol), palladium acetate (21 mg, 0.092 mmol), (±)-2,2′-bis(diphenylphosphino)-1,1′-binaphthalene (86 mg, 0.14 mmol) and cesium carbonate (900 mg, 2.76 mmol) in toluene (10 mL) under nitrogen was heated at 100° C. for 16 hours. After cooling to ambient temperature, the mixture was concentrated and the residue was diluted with dichloromethane (300 mL), washed with water and brine, dried over sodium sulfate, filtered and concentrated. The residue was purified by flash chromatography on silica gel (200-300 mesh) eluting with 5/1 petroleum ether/ethyl acetate to give the title compound.

Provenance & Evidence