Current Organic Chemistry - Volume 30, Issue 6, 2026

Asymmetric catalysis has witnessed remarkable progress in recent decades, due to the importance of chiral compounds, which play a pivotal role in numerous contemporary fields. Catalytic enantioselective C-C bond formation is an efficient method for constructing a variety of chiral molecules. Copper-catalyzed asymmetric allylic alkylation stands out as one of the most effective and appealing approaches within this category. This review comprehensively summarizes representative examples of asymmetric allylic alkylation catalyzed by copper, involving organometallic reagents over the last few decades, and classifies them according to the type of organometallic reagents, such as organomagnesium and organolithium compounds.

This comprehensive review outlines the multifaceted applications of pyrazolines and benzimidazoles, encompassing their discovery, synthetic methodologies, patent landscape, and clinical trial outcomes, with a focus on pyrazoline-benzimidazole or pyrazole-benzimidazole derivatives. This review highlights the synthesis and biological evaluation of pyrazoline-bearing benzimidazoles obtained through the reaction of benzimidazoles with substituted pyrazolines/pyrazoles. The synthesized compounds demonstrated a broad spectrum of pharmacological activities, including antimicrobial, antibacterial, antitubercular, antimalarial, anthelmintic, antiproliferative, anticancer, antinociceptive, antihistaminic, antiulcer, etc. Research on pyrazoline and benzimidazole derivatives constitutes a dynamic field, expanding the research domain within pharmaceutical chemistry and offering potential therapeutic solutions for various diseases.

Triazine is a heterocyclic aromatic ring that is divided into three isomers by nitrogen atom positions. 2-Aza-2-desamino-5,8-dideazafolic acid and 2-azaadenosine are 1,2,3-triazine derivatives, whereas azaribine, tirapazamine, lamotrigine, and 6-azacytosine are 1,2,4-triazine derivatives. Natural antibiotics like fervenulin, reumycin, and toxoflavin have a triazine ring structure. Ammeline, aceto-guanide, acetoguanamine, cyanuric acid, and melamine all include 1,3,5-triazine isomer or s-triazine as a lead structure. Hexamethylmelamine (altretamine), atrazine, cycloguanil, and almitrine are examples of s-triazine-containing medications. Triazines are important in pharmaceutical chemistry because they exhibit a wide range of pharmacological actions, making them valuable for drug design and development. Some triazine analogs have recently been tested in clinical trials, which might lead to more powerful medications and have fewer adverse effects than currently available pharmaceuticals. This article discusses the biological significance and synthesis of several triazine derivatives derived from heterocyclic and Triazine-containing medicines.

Nitrogen-containing heterocycles play a crucial role in medicinal chemistry and drug discovery, as several anticancer FDA-approved medicines are based on these compounds. Their structural and biological properties significantly impact their anticancer activity. Pyrazole and pyrimidine scaffolds show great anticancer potential. This review summarizes the synthesis and anticancer activity of several pyrazole and pyrimidine-based compounds, which exhibit great potential as cancer treatment candidates. The structural and biological characteristics of pyrazole and pyrimidine rings make them suitable scaffolds for designing novel anticancer agents. This review describes various synthetic routes for the preparation of pyrazole and pyrimidine derivatives, as well as their mechanisms of action in cancer therapy. These compounds exhibit potent cytotoxicity against breast, lung, and colon cancer cell lines. A detailed synthesis scheme shows how to incorporate pyrazole and pyrimidine scaffolds into medicinal compounds. Recent studies suggest that these derivatives exhibit substantial antitumor effects, supporting their development as targeted cancer therapies. Through the detailed description of synthesis, mechanisms of action, and anticancer activity, this review provides useful information on pyrazole and pyrimidine derivatives as potential future anticancer agents, highlighting their therapeutic potential in cancer treatment.

Indole derivatives possess a wide range of biological activities, including antibacterial, anti-inflammatory, analgesic, and anticancer properties. The Nenitzescu reaction is a valuable approach for their synthesis; however, there are challenges, such as the limited availability of dinitro derivatives and complex workup procedures, which necessitate optimization and improvement in practical efficiency. The Nenitzescu reaction is a versatile method for synthesizing hydroxyindoles, particularly 5-hydroxyindoles. 5-Hydroxyindoles play a crucial role as fundamental components in a wide range of natural chemicals and pharmaceuticals. This reaction has the potential to be applied in the fields of medicinal chemistry and natural product synthesis. The selection of catalysts, solvents, and temperature is a crucial factor in maximizing yields. Scientists have examined different solvents, catalysts, and reaction conditions in order to improve the output and effectiveness of the Nenitzescu process. The objective of this study is to examine the requirements for producing 5-hydroxyindoles by the Nenitzescu reaction. The study investigates the influence of catalysts, solvents, and reaction temperatures on the yield of the reaction. The main emphasis is on the Nenitzescu reaction, with the objective of enhancing its practicality and environmental friendliness. Several trials using various solvents and catalysts are conducted. Nitromethane and acetic acid serve as effective solvents. The cyclization of hydroxy indoles is enhanced by zinc halides, specifically ZnCl2 or ZnI2.