Current Organic Chemistry - Volume 29, Issue 10, 2025

This review article explores the direct oxidation of primary alcohols into carboxylic acids, highlighting its importance in organic synthesis for producing valuable chemicals in a sustainable and efficient manner. Carboxylic acids are widely employed in a wide range of applications, encompassing food preservatives, insecticides, dye intermediates, coatings, plasticizers, spices, flavors, scents, and a variety of industries such as polymers, solvents, and medications. This review article covers recent advancements in catalytic systems, including catalysts based on transition metals, organocatalysts, nanocatalysts, and electrochemical methods. It examines the impact of reaction conditions such as solvents, temperature, and substrate scope on these processes. The review also delves into mechanistic insights and recent developments in tandem and cascade reactions, aiming to provide a comprehensive understanding of current strategies and future research directions in this field.

Coumarins are a vital class of compounds recognized for their significant therapeutic potential, both in their natural forms and as synthetic derivatives. Characterized by a benzene ring fused to an α-pyranose ring, coumarins have garnered considerable attention from the scientific community due to their diverse pharmacological activities. This review article highlights the importance of coumarin hybrids, showcasing their enhanced biological properties and reactivity compared to traditional coumarin structures. We explore the pharmacological profiles of various coumarin derivatives, including their anti-cancer, anti-inflammatory, antiviral, antioxidant, antibacterial, and anti-tuberculosis activities, among others. The review examines how the incorporation of different functional groups on the coumarin scaffold can modulate its effectiveness against various diseases, particularly cancer. Furthermore, we discuss promising results from coumarin-based hybrids, such as coumarin-pyridine, coumarin-uracil, and coumarin-quinoline derivatives, demonstrating their efficacy against a range of pathogens. This comprehensive overview serves as a valuable resource for researchers interested in the potential of coumarin derivatives in therapeutic applications.

A series of sixteen new 4-(substituted phenyl)-6-(substituted phenylamino)-3,4-dihydropyrimidine-2(1H)-one/thione derivatives have been synthesized in two-step reaction. In the first step, chalcones (I1-I6) were obtained, and in the second step, these chalcones were reacted with urea and thiourea in the presence of potassium hydroxide to obtain the corresponding pyrimidinones and thiopyrimidinones. The progress of reaction was monitored by means of TLC (visualized it in Iodine chamber), The structures of the synthesized compounds 4-(substituted phenyl)-6-(substituted phenylamino)-3,4-dihydropyri-midine-2(1H)-ones/thione derivatives were investigated by IR, mass, ¹H-NMR spectral and elemental analysis. The title compounds were evaluated for anti-inflammatory and antioxidant activity. Anti-inflammatory activity in vivo was carried out using the carrageenan-induced rat-paw edema method and compared with standard drug diclofenac sodium. Antioxidant activity was measured using the DPPH, FRAP, and hydrogen peroxide (H2O2) method and compared with standard ascorbic acid. Electron-donating groups showed better antioxidant activity than electron-withdrawing ones in both series. All the compounds exhibited good to moderate activity. Compound DHPM8 showed better antioxidant activity, and compound DHPM6 exhibited better anti-inflammatory activity, while compound DHPM11 showed minimum antioxidant as well as anti-inflammatory activities than other compounds. To better understand, molecular docking studies were performed. The molecular docking studies revealed that all synthesized compounds showed good receptor binding interaction in which compound DHPM9 had the highest docking score of 9.8 due to interaction with CYS36, PRO153, TYR130, GLY45, LEU152, ARG469, LYS468, and GLU465.

This study aimed to synthesize a total of seven halogenated amidostilbenes 3a-3f using the Heck cross-coupling method. The synthesized stilbenes underwent further reactions with Lewis acids, such as FeCl3 and SnCl4, resulting in imines 4 and indolines 5, respectively. The structure of all synthesized compounds was elucidated using FTIR, 1D- and 2D-NMR, XRD, and HRMS analysis. Furthermore, the mechanistic details underlying the formation of both imines and indolines were also discussed.