Cesium carbonate → HCID 86602700, compound

Participants

Reaction Conditions

Reaction Steps

A mixture of (2R)-1-[3,5-bis(trifluoromethyl)benzoyl]-2-(4-methyl-3-trifluoromethanesulfonyloxybenzyl)-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]piperazine (0.10 g), benzophenone imine (30.5 mg), cesium carbonate (62 mg), palladium acetate (3 mg), and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (12.7 mg) in toluene was stirred at 80° C. under nitrogen atmosphere for 22 hours. After cooling, water and ethyl acetate were added to the mixture and the organic layer was separated, washed with brine, dried over sodium sulfate, and evaporated in vacuo. The residue was purified by column chromatography on silica gel (NH-DM1020, Fuji Silysia Chemical Ltd.) with a mixture of hexane and ethyl acetate (3:1) as eluent to give (2R)-1-[3,5-bis(trifluorometh yl)benzoyl]-2-[3-(diphenylmethyleneamino)-4-methylbenzyl]-4-[2-[(2S)-2-(methoxymethyl)morpholino]ethyl]piperazine (75 mg) as an oil.

Provenance & Evidence