COPPER(I)-CATALYZED DIRECT ARYLATION OF 1,4-DISUBSTITUTED 1,2,3-TRIAZOLES WITH ARYL IODIDES

Treatment of 1,4-disubstituted 1,2,3-triazoles with aryl iodides in the presence of a catalytic amount of copper chloride and lithium tert-butoxide (stoichiometric) in DMF at 140 degrees C leads to arylation at the 5-position. Various combinations of substituted aryl iodides and 1,4-disubstituted 1,2,3-triazoles bearing functional groups were found to be compatible.