Abstract
2,3-Dihydroquinazolin-4-one (DHQ) belongs to the class of nitrogen-containing heterocyclic compounds representing a core structural component in various biologically active compounds. In the past decades, several methodologies have been developed for the synthesis of the DHQ framework, especially the 2-substituted derivatives. Unfortunately, multistep syntheses, harsh reaction conditions, and the use of toxic reagents and solvents have limited their full potential as a versatile fragment. Recently, use of green chemistry and alternative strategies are being explored to prepare diverse DHQ derivatives. This fragment is used as a synthon for the preparation of biologically active quinazolinones and as a functional substrate for the synthesis of modified DHQ derivatives exhibiting different biological properties. In this review, we provide a comprehensive assessment of the synthesis and biological evaluations of DHQ derivatives.
Highlights
View Article Online2,3-Dihydroquinazolin-4-one (DHQ) belongs to the class of nitrogen-containing heterocyclic compounds representing a core structural component in various biologically active compounds
Nitrogen-containing heterocyclic scaffolds are quite common fragments in drugs and biologically active compounds.[1,2] The 2,3-dihydroquinazolin-4(1H)-one (DHQ) is an important aDepartment of Pharmacy, Health and Nutritional Sciences, University of Calabria, Ed
Some asymmetric strategies have been attempted, the aminal chiral center is sensitive to racemization, making it difficult to Mariateresa Badolato is currently pursuing her PhD degree in Translational Medicine under the supervision of Dr Francesca Aiello and Professor Antonio Garofalo at the University of Calabria, Italy
Summary
2,3-Dihydroquinazolin-4-one (DHQ) belongs to the class of nitrogen-containing heterocyclic compounds representing a core structural component in various biologically active compounds. Several methodologies have been developed for the synthesis of the DHQ framework, especially the 2substituted derivatives. Multistep syntheses, harsh reaction conditions, and the use of toxic reagents and solvents have limited their full potential as a versatile fragment. Use of green chemistry and alternative strategies are being explored to prepare diverse DHQ derivatives. This fragment is used as a synthon for the preparation of biologically active quinazolinones and as a functional substrate for the synthesis of modified DHQ derivatives exhibiting different biological properties. We provide a comprehensive assessment of the synthesis and biological evaluations of DHQ derivatives
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