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Chemical Insights into the Synthetic Chemistry of Quinazolines and Quinazolinones: Recent Advances

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Heterocycles occupy a central position in organic chemistry and are of particular interest largely due to their multifarious agrochemical and medicinal applications. Indeed, the importance of these compounds is clearly evident from their widespread prevalence in the chemical structures of marketed drugs and ...

Heterocycles occupy a central position in organic chemistry and are of particular interest largely due to their multifarious agrochemical and medicinal applications. Indeed, the importance of these compounds is clearly evident from their widespread prevalence in the chemical structures of marketed drugs and with particular reference to the pharmaceutical industry, heterocyclic motifs are especially prevalent with over 60% of the top retailing drugs containing at least one heterocyclic nucleus as part of the overall topography of the compound. In this context, nitrogen-containing heterocycles, particularly quinazolines and quinazolinones hold a very prominent position due to their diverse pharmacological profile. In addition, a variety of synthetic methods offering a facile, operationally simple and high yielding access to these motifs raise the interest level of synthetic and medicinal chemists to continually explore the new avenues affording drug-like molecules based on these entities.

The purpose of this collection is to publish high quality research and to identify new opportunities and explore recent developments in the library of quinazolines and quinazolinones that could potentially be employed in the design of medicinally relevant drug discovery approaches. In addition, the presented research will showcase the potential of quinazoline and quinazolinone derivatives as privileged motifs which can be accessed through a variety of synthetic efforts/methodologies starting from cheap and readily available starting materials. Although several methodologies have been developed to access these motifs, some limitations still exist for several methods due to the use of harsh reaction conditions and restricted substrate generality. The scope of some described reactions needs to be expanded. It is also highly desirable to focus on developing more eco-friendly processes which are in accordance with the green chemistry protocols. For medicinal purposes, one important strategy is to employ some functional groups or structural fragments that are helpful for improving physicochemical properties and affinity with target sites to modify clinical drugs. In general, the newly developed methods will not only broaden the synthetic chemistry scope of these scaffolds but also identify the structurally novel types of quinazoline and quinazolinone derivatives for all possibly medicinal applications.

We invite authors to contribute original research articles as well as reviews to this collection. Potential topics related to quinazolines and quinazolinones include, but are not limited to:

• New emerging protocols for the preparation of quinazolines and quinazolinones
• New carbon-heteroatom (C–X) bond formation.
• Key theoretical and mechanistic investigations
• New eco-friendly protocols
• Metal-free synthesis
• Free radical chemistry
• New sustainable methodologies
• Synthesis of new medicinal agents


Keywords: Heterocycles, Quinazolines, Quinazolinones, Synthetic methods, Medicinal applications


Important Note: All contributions to this Research Topic must be within the scope of the section and journal to which they are submitted, as defined in their mission statements. Frontiers reserves the right to guide an out-of-scope manuscript to a more suitable section or journal at any stage of peer review.

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