A highly active, air-stable, and versatile procedure for Buchwald–Hartwig and Sharpless–Meldal
C–N bond formation is reported. Under nearly solvent-free conditions using copper(II)
acetate and 2-phenyl-2-(4-phenyl-1H-1,2,3-triazol-1-yl)ethanol, a variety of N-heterocycles and various cyclic and noncyclic
secondary amines were arylated to form N-aryl compounds in moderate to excellent yields.
This methodology also provides rapid access to diverse 1,4-disubstituted 1,2,3-triazoles
in good to excellent yields. All reactions are performed in short times under air.
Key words
2-phenyl-2-(4-phenyl-1
H-1,2,3-triazol-1-yl)ethanol - Buchwald–Hartwig reaction - Sharpless–Meldal reaction
- copper catalysis - N-arylation