Executive Summary : | Small-ring heterocycles are found in a variety of natural products and bio-active compounds. Among them, nitrogen-containing heterocycles have a greater impact due to their extensive pharmacological applications. Aziridine, azetidine, pyrrolidine, etc., are belongs to small size saturated N-heterocycles. The synthetic utility and applications of highly strained three-membered aziridines are well studied in the literature with respect to the opening of the ring via C-N bond cleavage by nucleophiles and various transition metal catalysts due to high strain. The ring strain in four-membered saturated N-heterocycle, azetidines is lies between highly reactive three-membered aziridine and unreacted five-membered pyrrolidine. Due to this, less attention was made towards the ring-opening cross-coupling reactions of four-membered azetidines in comparison to three-membered aziridines to make C-C, C-heteroatom bonds. In this context, the development of deconstructive functionalization of azetidines would be useful in the synthesis of bio-active γ-functionalized alkylamine/amino acid scaffolds. Further substrate-controlled C-H activation of azetidines having bidentate ligand would give the library of densely functionalized and structurally diverse four-membered azetidine ring molecular architectures having significant pharmacological interest. |