Abstract

Dr. A. A. Patil*, P. R. Jain and D. V. Nagarale

ABSTRACT

N- Aryl amines and heterocycles are an important class of compounds and are widely used as medicinal[1] as analgesic drugs, biological[2] and NHC chemistry. Some of the compounds have also been reported as antibacterial. N-Aryl heterocycles like imidazole, benzimidazole, benzotriazole, pyrazole and indazole serves as important building blocks in pharmaceuticals. Some of the N-heterocyclic moiety is also found in many bioactive natural products. In addition 1-aryl benzotriazole are useful intermediates in the synthesis of pyridoacridine and carbolin synthesis. Among the heterocyclics, N-aryl imidazole is widely studied because of its distinct biomedical properties like AMPA receptor antagonists. Transition metal mediated C-N bond formations are important fundamental transformations and are commonly used for N-arylation reactions by metals such as Pd, Cu/CuI, and Fe. Mostly C-N bond formed by copper mediated (Ullmann reaction) and Palladium catalyzed (Buchwald-Hartwig reaction) has received much attention. Recently, iron catalyzed N-arylation of N-nucleophiles with various copperchelating ligands such as 1,10-phenoanthroline and vicinal diamines. N-arylation with excess of bases (K2CO3, K3PO4, KOH) in polar solvents (DMF, DMSO) was used in various literatures.