2-Azetidinone skeleton is well established as the pharmacophore of β-lactam antibiotics. β-lactam antibiotics are the most widely employed class of antibiotics. The structural diversity of biologically active β-lactam antibiotics led to the development of many novel methods for the construction of appropriately substituted azetidine with attendant control of functional group and stereochemistry. Azetidine derivatives are reported to show a variety of antimicrobial, antitubercular, anticonvulsant, anti-inflammatory and cardiovascular activities. These activities showed that the minor change in the substitution pattern activities of azetidine derivatives have enhanced dramatically.