Abstract:
Facile and metal-free syntheses of natural and natural product-inspired bioactive heterocycles are of paramount importance in drug discovery program; therefore, it is highly desirable to develop efficient protocols to generate a diverse library of drug-like molecules. In recent years, organohypervalent iodines have played a vital role as eco-friendly recyclable reagents to construct a variety of bioactive heterocycles, particularly with five- and six-membered ring systems. Due to readily accessible, easy-to-use and shorter reaction times, organohypervalent iodine reagents have gained special attention as versatile and benign oxidants in several organic transformations. Moreover, in a multistep synthesis of natural bioactive heterocycles, organohypervalent iodine reagents are important source to achieve key intermediates for being safer alternatives to hazardous and metal-based reagents. This chapter summarizes the recent trends adapted by organic chemists mainly in the synthesis of biologically relevant five- and six-membered heterocycles using such diverse organohypervalent iodine reagents.