Potassium Phosphate, Tribasic → HCID 87827837, compound

Participants

Reaction Steps

The mixture of 306 mg of 3-{(1S)-1-[(t-butoxycarbonyl)amino]ethyl}phenyl trifluoromethanesulfonate (synthesized according to a method disclosed in J. Med. Chem. 2004, 47, 2887-2896), 181 mg of 2,2,2-trifluoro-1-piperazin-1-yl-ethanone, 47.6 mg of tris(dibenzylideneacetone)(chloroform)dipalladium (0), 49.4 mg of 2-(di-t-butylphosphino)biphenyl, 246 mg of tripotassium phosphate, and 4 mL of toluene, was stirred overnight at 100° C. After cooling the reaction mixture back to room temperature, a saturated aqueous solution of sodium hydrogen carbonate was added thereto, and was extracted with ethyl acetate. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate, and the insolubles were filtered. The filtrate was concentrated under reduced pressure and purified by silica gel column chromatography, to obtain 277 mg of t-butyl((1S)-1-{3-[4-(trifluoroacetyl)piperazin-1-yl]phenyl}ethyl)carbamate [128-1] as a brown oily product.

Provenance & Evidence