One-Pot Facile Synthesis of Exclusive N1-Alkyl Benzotriazoles through Intramolecular Cyclization

The drawbacks associated with common synthetic approaches for N1-substituted benzotraizoles like involvement of unstable benzyne intermediate, low reaction yields, strictly anhydrous conditions and moreover the hazardous nature of low molecular weight azides prompted us to search a simple, short, and high yielding methodology to generate diverse N1-substituted benzotriazoles. Herein, a facile and high yielding protocol for diverse N1-alkyl/aryl benzotriazoles through intramolecular cyclization of different N-alkyl o-phenylenediamine/o-chloro-1,2,3-benzotriazenes under the catalysis of NaOAc.3H2O/CuI has been devised.