A chemical method for the preparation of nonprotected tryptophan via nickel(II) complexes under simple operating conditions was established. The carefully designed nickel(II) glycinates are inexpensive and can be quantitatively recovered releasing the target tryptophans in high yield. The method has a wide range of synthesis generality, allowing the preparation of various substituted tryptophans. Furthermore, the scalability of this method bodes well for its synthetic use as a general approach to biologically interesting tailor-made tryptophans and related compounds.
This review manuscript examines magnetic nanocatalysts and their pivotal role in forming carbon-sulfur (C-S) and carbon-selenium (C-Se) bonds. The study delves into the latest advancements in the synthesis, characterization, and application of magnetic nanocatalysts, highlighting their unique advantages, including enhanced catalytic activity, superior selectivity, and easy recovery through magnetic separation, which align with the principles of green chemistry. Through a critical analysis of recent research findings, this review also explores the mechanistic pathways facilitated by these nanocatalysts, offering insights into their operational efficiency and potential for recyclability. The manuscript aims not only to catalog the current achievements in this burgeoning field but also to identify challenges and propose future directions for developing more efficient, sustainable, and versatile catalytic systems for C-S and C-Se bond formation. By encompassing a broad spectrum of magnetic nanocatalysts, ranging from bare magnets to functionalized and composite materials, this review is a comprehensive resource for researchers engaged in organic synthesis, catalysis, and sustainable chemistry.
Benzo-fused γ-lactams are fundamental in medicinal chemistry, acting as essential elements for various therapeutic agents due to their structural adaptability and capability to enhance biological activity. In their synthesis, transition metals play a pivotal role as catalysts, offering more efficient alternatives to traditional methods by facilitating C–N bond formation through mechanisms like intramolecular coupling. Recent advances have especially spotlighted transition-metal-catalyzed C–H amination reactions for directly converting C(sp2)–H to C(sp2)–N bonds, streamlining the creation of these compounds. Furthermore, biocatalytic approaches have emerged, providing asymmetric synthesis of lactams with high yield and enantioselectivity. This review examined the transition metal-catalyzed synthesis techniques for producing benzo-fused γ-lactams, marking a significant leap in organic synthesis by proposing more effective, selective, and greener production methods. It serves as a valuable resource for researchers in the fields of transition metal catalysts and those engaged in synthesizing these lactams.
Benzimidazoles and 2,3-dihydroquinazolin-4(1H)-ones are of great interest in medicinal chemistry for their potential to develop new therapeutic agents. This research presents an innovative one-pot synthesis method for these compounds using indium oxide nanoparticles (In2O3 NPs) as a catalyst, which has shown consistent efficiency and reusability over seven cycles. Glycerol is used as an environmentally friendly solvent under mild conditions. The study demonstrates that various substituents on the benzene ring do not affect reaction efficiency, resulting in high product yields. Indium oxide nanoparticles outperform previous catalysts, often leading to lower yields and longer reaction times while less reusable. The catalyst was characterized using techniques such as FT-IR, BET, TEM, XRD, and TGA, confirming its retained activity after multiple uses.
The synthesis of imidazolines has gained significant attention due to their wide range of applications in pharmaceuticals, agrochemicals, and materials science. Recent advancements in the use of transition metal catalysts have revolutionized the methodologies for synthesizing these heterocyclic compounds. This review highlights the latest developments in transition metal-catalyzed reactions, focusing on their efficiency, selectivity, and sustainability. Key breakthroughs include the utilization of palladium, nickel, and copper catalysts, which have demonstrated remarkable activity in various coupling and cyclization reactions. Additionally, the incorporation of green chemistry principles has led to more environmentally friendly processes. The mechanistic insights and practical applications discussed herein provide a comprehensive understanding of the current state and future prospects of transition metal-catalyzed imidazoline synthesis. This review highlights the literature from 2010 to 2024, focusing on various protocols involving transition metal catalysts for the synthesis of diverse imidazoline heterocyclic compounds.
The synthesis of benzoxazoles, a class of heterocyclic compounds with broad applications in pharmaceuticals, agrochemicals, and materials science, has gained considerable attention due to their The synthesis of benzoxazoles, a class of heterocyclic compounds with broad applications in pharmaceuticals, agrochemicals, and materials science, has gained considerable attention due to their diverse biological and functional properties. Magnetic catalysts have emerged as a versatile and sustainable approach for preparing benzoxazoles, offering several advantages, including enhanced catalytic activity, reusability, and ease of separation. This review highlights the recent advancements in the design and application of magnetic catalysts in benzoxazole synthesis, emphasizing their role in promoting green and efficient chemical transformations. The discussion explores their mechanistic aspects, synthetic versatility, environmental benefits, and potential integration into continuous flow systems and hybrid catalytic processes. The application of magnetic catalysts not only addresses the challenges of traditional synthetic methods but also paves the way for eco-friendly and scalable approaches to benzoxazole production. After separation, these catalysts can be recovered and reused in multiple-reaction cycles without significant activity loss. This review emphasizes the role of magnetic catalysts in synthesizing benzoxazoles, highlighting their ability to enhance traditional synthetic methods into sustainable, high-yield, and scalable processes. Integrating magnetic catalysis into benzoxazole synthesis represents a significant step forward in achieving greener, more efficient methodologies in heterocyclic chemistry.
Organosilicon chemistry is a valuable branch of chemistry science, particularly in organic synthesis, because compounds containing carbon–silicon (C–Si) bonds are valuable in various fields such as pharmaceuticals, agrochemicals, and materials science. Copper catalysts have emerged as a pivotal tool in the formation of carbon–silicon bonds, offering a sustainable and efficient alternative to traditional methods. The use of copper in catalyzing these reactions is advantageous due to its abundant availability and cost-effectiveness compared to other precious metals. Recent advancements have demonstrated that copper-catalyzed reactions are not only versatile but also exhibit high degrees of regio- and enantioselectivity, making them highly desirable for complex organic synthesis. The ability of copper to facilitate the formation of C(sp3)–Si bonds is particularly noteworthy, as these bonds are integral in the development of pharmaceuticals and in the synthesis of silicon-containing organic compounds, which are valuable in materials science. Moreover, the mild reaction conditions, coupled with the low toxicity of copper catalysts, align well with the principles of green chemistry, further underscoring the benefits of this approach. This review outlines the recent applications of copper catalysts (from 2010 to 2024) in the preparation of organosilicon compounds by substitution reactions and by addition reactions to imine, aldehyde and C=C double bonds.
This manuscript introduces a groundbreaking study on the development and application of magnetically recoverable catalysts for the efficient multicomponent synthesis of organosulfur compounds. Capitalizing on the unique advantages of magnetic recovery, these catalysts streamline the synthesis process, offering an innovative solution that marries efficiency with environmental sustainability. By facilitating the multicomponent reaction of key precursors in the presence of sulfur sources, the catalysts enable the straightforward synthesis of various valuable organosulfur compounds, crucial in numerous pharmaceutical, agricultural, and material science applications. Key findings demonstrate a significant enhancement in reaction yields and selectivity and the remarkable ease with which the catalysts can be recovered and reused, thereby reducing both waste and operational costs. Magnetic catalysts, often based on magnetic iron nanoparticles, facilitate rapid and efficient reactions under mild conditions, offering superior atom economy, reduced solvent use, and the potential for scalable processes. Additionally, magnetically separating the catalysts from the reaction mixture enables multiple recycling cycles, reducing waste and operational costs. The review also discusses the mechanistic insights, challenges, and recent advancements in this field alongside future directions for developing more robust and versatile magnetic catalytic systems. This research embodies a significant step forward in the field of catalysis, highlighting the potential of magnetically recoverable catalysts to revolutionize the synthesis of complex molecules. Future perspectives discussed in the manuscript focus on expanding the scope of these catalysts to broader applications, optimizing catalyst design for enhanced performance, and further aligning chemical synthesis processes with the principles of green chemistry. This review covers the literature from 2010 to the end of 2024, and it encompasses the different one-pot protocols for synthesizing various heterocyclic organosulfur compounds based on magnetically recoverable catalysts.
In the last 10 years, the synthesis of anthracene scaffolds has attracted considerable interest because of their distinctive electronic characteristics and various uses in organic electronics, photovoltaics, and therapeutics. Anthracene, a polycyclic aromatic hydrocarbon, is valued for its lightweight, stability, and electron transport capabilities, making it a key building block in advanced materials. Traditional synthesis methods often face challenges such as low selectivity and harsh conditions. However, recent advancements in transition metal-catalyzed reactions have transformed the field, offering more efficient and versatile approaches. This review examines methodologies utilizing transition metal catalysts like palladium, zinc, indium, cobalt, gold, iridium, rhodium and ruthenium, which have enabled novel synthetic pathways and selective formation of substituted anthracenes through cross-coupling reactions. The function of ligands, including phosphines and N-heterocyclic carbenes, in improving reaction efficiency and selectivity is also examined. The shift towards greener methodologies is noted, with a focus on minimizing waste and reducing toxic reagents. The shift towards greener methodologies is noted, with a focus on minimizing waste and reducing toxic reagents. Several case studies demonstrate the successful application of these techniques, highlighting the structural diversity and functional potential of anthracene derivatives in various applications.
The unique reactivity and beneficial features of the 5-aminotetrazole synthon (1H-tetrazol-5-amine) have made it a versatile and effective building block in the synthesis of heterocyclic compounds. In addition, several drugs containing this scaffold with a wide array of biological properties have been already introduced. Heterocyclic structures are the backbone of many biologically active and industrially important compounds. 5-Aminotetrazole is one of the favored synthons used in the preparation of heterocycle-bearing compounds, especially in multicomponent synthesis. This review highlights a comprehensive overview of the emerging applications of 5-aminotetrazole as a key component in the synthesis of heterocyclic frameworks through multicomponent reactions, reported between 2017 and July 2023.
Heterocycles are an important class of compounds that are widely used in pharmaceuticals, agrochemicals, dyes, and materials. Multicomponent reactions (MCRs) offer efficient synthetic routes for producing these complex structures. The search for effective and sustainable catalytic processes in organic synthesis has led to the exploration of various nanomaterials as potential catalysts. To this end, carbon nanotubes (CNTs) have recently emerged as promising heterogeneous catalysts for the MCR synthesis of heterocycles due to their unique properties, which include high surface area and reactivity, tunable surface chemistry, excellent electrical conductivity, recyclability, and exceptional thermal and chemical stability. This review provides a comprehensive analysis and overview of the use of CNTs as catalysts for synthesizing heterocycles via MCRs and their advantages.
Ultrasonic irradiation serves as a vigorous and environmentally sustainable approach for augmenting multicomponent reactions (MCRs), offering benefits such as thermal enhancement, agitation, and activation, among others. Malononitrile emerges as a versatile reagent in this context, participating in a myriad of MCRs to produce structurally diverse heterocyclic frameworks. This review encapsulates the critical role of malononitrile in the sonochemical multicomponent synthesis of these heterocyclic structures. The paper further delves into the biochemical and pharmacological implications of these heterocycles, elucidating their reaction mechanisms as well as delineating the method's scope and limitations. We furnish an overview of the merits and challenges inherent to this synthetic approach and offer insights for potential avenues in future research.
Abstract This review provides an overview of the recent advances in the synthesis of diverse heterocyclic compounds using thiosemicarbazide as a key building block via multicomponent reactions. Thiosemicarbazide is a versatile reagent that has gained significant attention in organic synthesis due to its ability to participate in diverse multicomponent reactions for the efficient and sustainable construction and assembly of novel bioactive molecules and pharmaceuticals. This review discusses the potential applications and future directions in this rapidly evolving area of research. It provides valuable insights into the innovative approaches for the synthesis of heterocycles using thiosemicarbazide, showcasing its significance in modern organic chemistry research. In summary, this review provides an overview of the current state of the art, highlighting the use of thiosemicarbazide in the synthesis of novel heterocyclic compounds reported between 2015 and early 2024.
An efficient multicomponent reaction of newly designed β-trifluoromethyl β-diazo esters, acetonitrile, and carboxylic acids via an interrupted esterification process under copper-catalyzed conditions has been developed, which affords various unsymmetrical β-trifluoromethyl N,N-diacyl-β-amino esters in good to excellent yields. The reaction features mild conditions, a wide scope of β-amino esters and carboxylic acids, and also applicability to large-scale synthesis, thus providing an efficient way for the synthesis of β-trifluoromethyl β-diacylamino esters. Furthermore, this reaction represents the first example of a Mumm rearrangement of β-trifluoromethyl β-diazo esters.
Although radioactive experiments are necessary in radiopharmaceutical drug discovery and theranostic cancer research, they are expensive, require special facilities, and face certain restrictions. Thus, finding techniques not involving radioactivity is highly beneficial for minimizing these disadvantages in such research. In this regard, methods using inductively coupled plasma-mass spectrometry (ICP-MS) have emerged as viable alternatives to traditional radioactive approaches. Despite its potential, practical applications of ICP-MS in radiopharmaceutical cancer research have only emerged in recent years. This Perspective focuses on the development and implementation of nonradioactive ICP-MS-based assays in radiopharmaceutical research and aims to inspire future research efforts in this area.
Cancer is one of the leading causes of death globally and it stands at second place after cardiovascular disease. About one in five of us will die of cancer and the high mortality rate of this disease is due to the lack of prevention, diagnosis, and treatment. Many researchers all around the world are working on the development of novel anticancer drugs with different mechanisms of action. Coumarin is a highly promising pharmacophore for the development of novel anticancer drugs. Not only that, hybridization of this moiety with other anticancer pharmacophores emerges as a potent breakthrough in the treatment of cancer in order to decrease the side effects and increase efficiency. This review will aim to provide an overview of the recent development of coumarin derivatives as novel anticancer drugs, covering articles published between 2015 and 2022, along with their mechanisms of action and structure-activity relationship studies.
Abstract Heterocycles are a vital class of compounds in numerous fields, including drug discovery, agriculture, and materials science. Efficient methods for the synthesis of heterocycles remain critical for meeting the demands of these industries. Recent advances in multicomponent reactions (MCRs) utilizing 2‐aminobenzothiazole (ABT) have shown promising results for the formation of heterocycles. The versatility of 2‐aminobenzothiazole in this context has enabled the rapid and efficient construction of diverse heterocyclic structures. Various synthetic methodologies and reactions involving 2‐aminobenzothiazole are discussed, highlighting its importance as a valuable building block in the synthesis of complex heterocycles. The potential applications of these heterocycles in drug discovery and material science are also explored. Overall, this review provides a comprehensive overview of the current state of research in the field and offers insights into the future directions of this promising area of study. We highlight the potential of ABT as a versatile and sustainable starting material in heterocyclic synthesis via MCRs, with significant implications for the chemical industry.
Spiro heterocycle frameworks are a class of organic compounds that possesses unique structural features making them highly sought-after targets in drug discovery due to their diverse biological and pharmacological activities. Microwave-assisted organic synthesis has emerged as a powerful tool for assembling complex molecular architectures. The use of microwave irradiation in synthetic chemistry is a promising method for accelerating reaction rates and improving yields. This review provides insights into the current state of the art and highlights the potential of microwave-assisted multicomponent reactions in the synthesis of novel spiro heterocyclic compounds that were reported between 2017 and 2023.