反应详情

温度

70 °C

To a solution of tert-butyl (2R,5R)-5-(azidomethyl)-2-[2-(2-{[N-(methoxycarbonyl)-β-phenyl-L-phenylalanyl]amino}phenyl)ethyl]morpholine-4-carboxylate (1 eq.) in tetrahydrofuran (0.033M) were added phenylacetylene (3.9 eq.) and Hunig's base (5 eq.). Nitrogen was then bubbled for 5 minutes through the reaction mixture which was placed in a sealed tube. Copper(I) iodide (1.5 eq.) was added to the reaction mixture and the temperature was raised to 70° C. for 16 hrs. The reaction mixture was evaporated to dryness and the evaporation residue was purified by automated silica gel flash chromatography system eluted with a gradient 0% to 10% of MeOH/CH2Cl2.

1. customNitrogen was then bubbled for 5 minutes through the reaction mixture which
2. customwas placed in a sealed tube
3. customThe reaction mixture was evaporated to dryness
4. customthe evaporation residue was purified by automated silica gel flash chromatography system
5. washeluted with a gradient 0% to 10% of MeOH/CH2Cl2