Sulfoximine and its congeners are a versatile class of structural motifs widely found in a plethora of pharmaceutical compounds and crop protection industries due to their fascinating structural architecture. Former discoveries nicely demonstrates the synthetic routes of unmasked and various N-functionalized sulfoximines but recent efforts from the synthetic community have divulged the applicability of sulfoximine analogue as reusable and transformable DG (directing group) to fabricate multifunctionalized (Het)arenes and enhance the bioactivities. Considering the synthetic potentiality and great influence of this scaffold, we provide a summary of NÀ H/CÀ H functionalization strategies of sulfoximine and application (as a directing group) with special emphasis on the mechanistic underpinnings. Additionally, we also hoped that this comprehensive review article (up to midst of 2020) will be useful for synthetic researchers and medicinal chemists and will inspire for further novel chemical transformations in this arena.

Quinazolinone and its derivatives are an important class of heterocyclic scaffolds in pharmaceuticals and natural products. This review provides the recent research advances in the transition metal catalyzed selective C–H bond functionalization of quinazolinone.

4‐Quinolone derivatives are serving as active components in diverse families of drugs such as antibacterial, antiviral, antimalarial, anticancer, antitumor and anti‐HIV agents. They have also attracted the significant attention in synthetic chemistry due to their prolific development, pharmacokinetic properties and good tolerability. Recent years have observed an upsurge in the modification of the 4‐quinolone scaffold. This review covers (2002 to 2019) the progress of the developments in the syntheses as well as functionalization of 4‐quinolones in different positions.

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Herein, we report the [Bis(trifluoroacetoxy)iodo]benzene mediated C−H bond arylselenylation of 4H‐Pyrido‐[1,2‐a]‐Pyrimidin‐4‐ones using readily available organodiselenides. This methodology is scalable and permits for the generation of a broad spectrum of functionally and structurally diverse selenoether derivatives in very promising yields (up to 98%). Notably, this protocol proceeds at ambient conditions and in the absence of a metal. The application of this methodology for the facile synthesis of ArSe substituted 5H‐thiazolo‐pyrido[3,2‐a]pyrimidin‐4‐ones is also demonstrated.