title: Microwave Assisted Synthesis of Biorelevant Benzazoles.
abstract: The benzazole scaffolds are present in various therapeutic agents and have been recognized as the essential pharmacophore for diverse biological activities. These have generated interest and necessity to develop efficient synthetic methods of these privileged classes of compounds to generate new therapeutic leads for various diseases. The biological activities of the benzazoles and efforts towards their synthesis have been summarized in a few review articles. In view of these, the aim of this review is to provide an account of the developments that have taken place in the synthesis of biorelevant benzazoles under microwave irradiation as the application of microwave heating has long been recognized as a green chemistry tool for speedy generation of synthetic targets. Attention has been focused to those literature reports wherein the use of microwave irradiation is the key step in the formation of the heterocyclic ring system or in functionalization of the benzazole ring system to generate the essential pharmacophoric feature. The convenient and economic way to synthesize these privileged class of heterocycles through the use of microwave irradiation that would be beneficial for the drug discovery scientist to synthesize biologically active benzazoles and provide access to wide range of reactions for the synthesis of benzazoles constitute the theme of this review. Examples have been drawn wherein the use of microwave heating offers distinct advantage in terms of improved product yields and reduction of reaction time as compared to those observed for the synthesis under conventional heating.
authors: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S. A. S. Nagar 160 062, Punjab, India.
authors: Kapileswar
authors: K
authors: Seth
authors: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S. A. S. Nagar 160 062, Punjab, India.
authors: Priyank
authors: P
authors: Purohit
authors: Department of Medicinal Chemistry, National Institute of Pharmaceutical Education and Research (NIPER), Sector 67, S. A. S. Nagar 160 062, Punjab, India.
authors: Asit K
authors: AK
authors: Chakraborti
mesh_terms: D001393:Azoles / Q000138:chemical synthesis* / Q000737:chemistry; D008872:Microwaves; D015394:Molecular Structure
chemical_list: D001393:Azoles
keywords: 2-Aminophenol; 2-aminothiophenol; aldehyde; benzimidazole; benzothiazole; benzoxazole; bio-activity; bis-heterocyclic scaffolds; carboxylic acids; catalyst-free reaction; conventional heating; domino reaction; fused ring system; green chemistry; michael reaction; microwave irradiation; multi-component reaction; one-pot
  reaction; ortho-phenylenediamine; solid-support; solvent-
  free reaction