The pyranopyrimidine core is a key precursor for medicinal and pharmaceutical industries due to its broader synthetic applications as well as its bioavailability. Among its four possible isomers, we found that 5H-pyrano[2,3-d]pyrimidine scaffolds have a wide range of applicability, and in recent years, they have been intensively investigated, but the development of the main core is found to be more challenging due to its structural existence. In this review article, we cover all of the synthetic pathways that are employed for the development of substituted 4-aryl-octahydropyrano/hexahydrofuro[2,3-d]pyrimidin-2-one (thiones) and 5-aryl-substituted pyrano[2,3-d]pyrimidindione (2-thiones) derivatives through a one-pot multicomponent reaction using diversified hybrid catalysts such as organocatalysts, metal catalysts, ionic liquid catalysts, nanocatalysts, green solvents, catalyst-/solvent-free conditions, and miscellaneous catalysts as well as the mechanism and recyclability of the catalysts. This review mainly focuses on the application of hybrid catalysts (from 1992 to 2022) for the synthesis of 5H-pyrano[2,3-d]pyrimidine scaffolds. This review will definitely attract the world's leading researchers to utilize broader catalytic applications for the development of lead molecules.

In the current study, we report the synthesis of novel 4-((1-((1H-1,2,3-triazole-4-yl)methyl)-1H-indol-3-yl)methylene)-5-methyl-2-phenyl-2,4-dihydro-3H-pyrazole-3-one derivatives 5a-o. The compounds were prepared through a Knoevenagel condensation reaction and copper-catalyzed azide-alkyne cycloaddition (CuAAC) Click chemistry approach. The synthesized compounds exhibited promising antimicrobial activity against both Gram-positive and Gram-negative bacteria. Compounds 5e, 5h, and 5i displayed potent activity with MIC value 10 μg/mL against Acinetobacter baumannii, in comparison to standard drugs chloramphenicol and ampicillin. Compounds 5d, 5h, 5i, 5l, 5m, and 5n exhibited good-to-moderate antifungal activity against Candida albicans and Aspergillus niger equivalent to standard drugs nystatin and fluconazole. In this study, the cytotoxicity profile of a series of compounds was assessed using SHSY-5Y cells. The results indicate that compounds 5a-o exhibit no significant cytotoxicity at concentrations up to 100 μg/mL, in comparison to both untreated and vehicle control groups. These findings highlight the safety and tolerability of compounds as well as the potential of the synthesized compounds as effective agents against bacterial and fungal infections.

Twenty-three new derivatives of (R/S)-TDHPM-5-carboxanilide have been synthesized with up to 99% yield. All racemates were separated using chiral HPLC (Prep LC) which provided up to 99.99% purity. AC was determined using circular dichroism spectra.

Herein, we demonstrate the synthesis of a bioactive novel series of alkoxy-functionalized dihydropyrimido[4,5-b]quinolinone derivatives using a multicomponent microwave-assisted reaction that exhibits potent antiproliferative and invasive activity.

This review highlights different synthetic strategies for preparing a spirocyclopropane moiety, covering the literature from 1989 to 2024. The spirocyclopropane moiety is a structural scaffold that is used to access synthetic libraries of highly functionalized spirocarbo- and heterocyclic molecules. The review showcases different routes for the synthesis of spirocyclopropanes that utilize distinct precursors and methodologies, including cascade reactions, cyclopropanation, Michael-initiated ring closure (MIRC), and one-pot and multicomponent synthesis. These discussions are organized around the oxindole core, which include isatin, oxindole, 3-chlorooxindole, and 3-alkenyl oxindoles. Additionally, this review explores various ylides and other techniques. The goal of this review is to provide a background for synthetic chemistry researchers to develop new ideas and novel synthetic routes to spirocyclopropanes. 1 Introduction2 Synthesis of Spirocyclopropanes from 3-Chlorooxindole Derivatives3 Synthesis of Spirocyclopropanes from Isatin Derivatives3.1 Synthesis of Spirocyclopropanes from Alkylidene Oxindole Derivatives3.2 Synthesis of Spirocyclopropanes from Diazooxindole Compounds4 Synthesis of Spirocyclopropanes from 1,3-Diones5 Synthesis of Spirocyclopropanes from N-Ylides6 Synthesis of Spirocyclopropanes from S-Ylides7 Miscellaneous Syntheses of Spirocyclopropanes8 Conclusion9 List of Abbreviations