Regioselective syntheses of fully-substituted 1,2,3-triazoles: the CuAAC/C-H bond functionalization nexus

Regioselective syntheses of 1,4,5-trisubstituted 1,2,3-triazoles were accomplished by three different strategies, relying on (i) the interception of stoichiometrically formed 5-cuprated-1,2,3-triazoles, (ii) the use of stoichiometrically functionalized alkynes or (iii) catalytic C-H bond functionalizations. This perspective article summarizes progress in this research area until June 2010. Regioselective syntheses of 1,4,5-trisubstituted 1,2,3-triazoles were accomplished by three different strategies, relying on (i) the interception of stoichiometrically formed 5-cuprated-1,2,3-triazoles, (ii) the use of stoichiometrically functionalized alkynes or (iii) catalytic C-H bond functionalizations.