Ethanol → HCID 21948278, compound

Participants

Reaction Steps

Diphenylphosphoryl azide (15.8 ml) was added to a mixture of 4-[[4-(benzyloxycarbonyl)-2-oxo-1-piperazinyl]methyl]-1-(tert-butoxycarbonyl)-4-piperidinecarboxylic acid (29 g) obtained in Reference Example 6, triethylamine (10.2 ml) and toluene (290 ml) at 0° C. under stirring, and the mixture was stirred at room temperature for 1 hour, and at 100° C. for 2 hours. Ethanol (290 ml) was added, and the mixture was heated under reflux for 12 hours, and concentrated under reduced pressure. The residue was purified by silica gel chromatography (hexane/ethyl acetate=1/3-ethyl acetate/methanol=10/1) to obtain the title compound (26 g, 82%) as pale yellow powders.

Provenance & Evidence