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Journal articles on the topic 'Heterocycles'

Author: Grafiati

Published: 4 June 2021

Last updated: 25 July 2025

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1

Zhu, Yannan, and You Huang. "Organocatalyzed [3+3] Annulations for the Construction of Heterocycles." Synthesis 52, no. 08 (2020): 1181–202. http://dx.doi.org/10.1055/s-0039-1690810.

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Six-membered heterocyclic systems are widely distributed in many natural products and pharmaceuticals, and the construction of highly functionalized six-membered heterocyclic compounds is an important topic in modern organic synthesis. Organocatalyzed [3+3] annulations represents an important method for assembling a substantial variety of six-membered cycles that contain one or more heteroatoms. This review describes the development of organocatalyzed [3+3] annulations for the synthesis of six-membered heterocycles, including organocatalysis using secondary amines, tertiary amines, phosphines,

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2

Andres, C. J., Derek J. Denhart, Milind S. Deshpande, and Kevin W. Gillman. "Recent Advances in the Solid Phase Synthesis of Drug Heterocyclic Small Molecules." Combinatorial Chemistry & High Throughput Screening 2, no. 4 (1999): 191–210. http://dx.doi.org/10.2174/1386207302666220204193145.

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Abstract: Because of their synthetic challenge, broad range of physical I chemical properties, and diverse biological activities, heterocycles continue to be of interest to both the academic and industrial chemist. This review covers recent advances in the solid phase synthesis of drug-like heterocyclic small molecules. Syntheses which form the heterocycle on the solid phase are emphasized; syntheses in which a preformed heterocycle is functionalized on the solid support have been omitted. The majority of references are from publication year 1999. This review should be of interest to anyone in

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3

Luna, Isadora Silva, Rayssa Marques Duarte da Cruz, Ryldene Marques Duarte da Cruz, Rodrigo Santos Aquino de Araújo, and Francisco Jaime Bezerra Mendonça-Junior. "1,4-Dithiane-2,5-diol: A Versatile Synthon for the Synthesis of Sulfur-containing Heterocycles." Current Organic Synthesis 15, no. 8 (2018): 1026–42. http://dx.doi.org/10.2174/1570179415666180821154551.

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Background: 1,4-Dithiane-2,5-diol (1,4-DTD) is the stable dimer of α-mercapto acetaldehyde. This commercially available ambidentade compound is characterized as having in its chemical structure one group that acts as an electrophile and another that acts as a nucleophile, this permits its use as versatile and efficient synthon in synthetic heterocycle procedures. Objective: The aim of this review is to present synthetic applications of 1,4-DTD in heterocyclic chemistry and their applicability to the synthesis of bioactive compounds. Conclusion: Gewald reactions to obtain C-4 and C-5 unsubstitu

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4

Winne, Johan, Jan Hullaert, Bram Denoo, Mien Christiaens, and Brenda Callebaut. "Heterocycles as Moderators of Allyl Cation Cycloaddition Reactivity." Synlett 28, no. 18 (2017): 2345–52. http://dx.doi.org/10.1055/s-0036-1588511.

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For the rapid elaboration of polycarbocyclic scaffolds, prevalent in many important families of terpenoid natural products, allyl cations derived from simple heterocyclic alcohols can be used as versatile reaction partners in both (4+3) and (3+2) cycloaddition pathways. Our recent progress in this area is outlined, pointing towards the untapped potential of heterocycles to act as reagents in novel or known but challenging organic transformations.1 Heterocyclic Reagents2 Cycloadditions and Allyl Cations3 Furfuryl Cations in Cycloadditions4 Heterocycle-Substituted Cations in Cycloadditions5 Mech

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5

Rusu, Aura, Ioana-Maria Moga, Livia Uncu, and Gabriel Hancu. "The Role of Five-Membered Heterocycles in the Molecular Structure of Antibacterial Drugs Used in Therapy." Pharmaceutics 15, no. 11 (2023): 2554. http://dx.doi.org/10.3390/pharmaceutics15112554.

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Five-membered heterocycles are essential structural components in various antibacterial drugs; the physicochemical properties of a five-membered heterocycle can play a crucial role in determining the biological activity of an antibacterial drug. These properties can affect the drug’s activity spectrum, potency, and pharmacokinetic and toxicological properties. Using scientific databases, we identified and discussed the antibacterials used in therapy, containing five-membered heterocycles in their molecular structure. The identified five-membered heterocycles used in antibacterial design contai

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6

Romero-Hernández, Laura L., Ana Isabel Ahuja-Casarín, Penélope Merino-Montiel, Sara Montiel-Smith, José Luis Vega-Báez, and Jesús Sandoval-Ramírez. "Syntheses and medicinal chemistry of spiro heterocyclic steroids." Beilstein Journal of Organic Chemistry 20 (July 24, 2024): 1713–45. http://dx.doi.org/10.3762/bjoc.20.152.

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There is compelling evidence that incorporating a heterocyclic moiety into a steroid can alter its pharmacological and pharmacokinetic properties, driving intense interest in the synthesis of such hybrids among research groups. In this review, we present an overview of recent synthetic methodologies, spanning the period from 2000 to 2023, for the preparation of spiro heterocyclic steroids. The compounds surveyed encompass four-, five-, six-, and seven-membered heterocycles appended to various positions of steroidal backbones, with spirocycles containing oxygen, nitrogen, and sulfur atoms being

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7

Slivka, Mikhailo, and Mikhailo Onysko. "The Use of Electrophilic Cyclization for the Preparation of Condensed Heterocycles." Synthesis 53, no. 19 (2021): 3497–512. http://dx.doi.org/10.1055/s-0040-1706036.

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AbstractCondensed heterocycles are well-known for their excellent biological effects and they are undeniably important compounds in organic chemistry. Electrophilic cyclization reactions are widely used for the synthesis of mono-heterocyclic compounds. This review highlights the utility of electrophilic cyclization reactions as an effective generic tool for the synthesis of various condensed heterocycles containing functional groups that are able to undergo further chemical transformations, such as nucleophilic substitution, elimination, re-cyclization, cleavage, etc. This review describes the

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8

Cui, Hai-Lei. "Recent Advances in DMSO-Based Direct Synthesis of Heterocycles." Molecules 27, no. 23 (2022): 8480. http://dx.doi.org/10.3390/molecules27238480.

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Besides serving as a low-toxicity, inexpensive and easily accessible solvent, dimethyl sulfoxide (DMSO) has also been extensively used as a versatile reagent for the synthesis of functionalized molecules. Dimethyl sulfoxide can not only be utilized as a carbon source, a sulfur source and an oxygen source, but also be employed as a crucial oxidant enabling various transformations. The past decade has witnessed a large number of impressive achievements on the direct synthesis of heterocycles as well as modifications of heterocyclic compounds by applying DMSO as a reagent. This review summarized

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9

Mr., Mayur Ashok Patkari, Roshan M. Chaudhari Mr., Hitendra S. Chaudhari Mr., and S. P. Pawar Dr. "A Review on Heterocyclic Compound Containing Anticancer Agent, As A Medicinal Chemistry Perspective." Journal of Advances in Clinical Pharmacology 2, no. 1 (2023): 27–38. https://doi.org/10.5281/zenodo.10279377.

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<i>One of the main causes of death in the globe is cancer. Cancer is caused by gene and protein regulation errors in cells. Despite their side effects, surgery, radiation therapy, and the use of anticancer drugs constitute the contemporary cancer therapy. Heterocyclic chemistry is the general field of study. The article's goal is to cover the most current developments in heterocyclic nitrogen compounds as potential cancer chemotherapeutic agents. Heterocyclics make up more than 80% of new medications, and those that contain nitrogen have better pharmacological effects than those that do not. C

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10

Ābele, E., R. Ābele, Ļ. Golomba, J. Višņevska, T. Beresņeva, and K. Rubina. "Oximes of Seven-Membered Heterocyclic Compounds Containing One Heteroatom." Latvian Journal of Chemistry 50, no. 3-4 (2011): 205–22. http://dx.doi.org/10.2478/v10161-011-0071-7.

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Oximes of Seven-Membered Heterocyclic Compounds Containing One Heteroatom Literature data on the synthesis and structure of azepane, oxepane and thiepane oximes were reviewed. Synthesis of novel heterocycles from oximes of seven-membered heterocycles containing one heteroatom were described. Biological activity of oximes of seven-membered heterocycles with one heteroatom was also reviewed.

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11

Ābele, E. "Oximes of Seven-Membered Heterocyclic Compounds Containing Two Heteroatoms." Latvian Journal of Chemistry 51, no. 1-2 (2012): 83–92. http://dx.doi.org/10.2478/v10161-012-0005-z.

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Oximes of Seven-Membered Heterocyclic Compounds Containing Two Heteroatoms Literature data concerning the synthesis and structure of diazepane, oxazepane and thiazepane oximes were reviewed. Synthesis of novel heterocycles from the oximes of seven-membered heterocycles containing two heteroatoms was described. Biological activity of oximes of seven-membered heterocycles with two heteroatoms was also reviewed.

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12

Lechel, Tilman, and Hans-Ulrich Reissig. "Synthesis of heterocycles via alkoxyallenes." Pure and Applied Chemistry 82, no. 9 (2010): 1835–44. http://dx.doi.org/10.1351/pac-con-09-09-06.

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Lithiated alkoxyallenes are very versatile components for the synthesis of heterocycles such as furans, pyrroles, and 1,2-oxazines, easily allowing the preparation of natural products via these heterocyclic intermediates. A surprising three-component synthesis of N-acylated enaminones allowed the synthesis of highly functionalized 4-hydroxypyridines, 5-acetyloxazoles, and pyrimidines. All these heterocyclic products are ready for further functionalizations, in particular for palladium-catalyzed reactions, leading to libraries of new interesting heterocycles.

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13

Deep, Aman, PrachI, and Hament Panwar. "THE CHEMISTRY OF HEALING: HETEROATOMIC DERIVATIZATION AND THEIR MEDICINAL APPLICATIONS." Annals of Science and Allied Research 2, no. 1 (2024): 26–37. https://doi.org/10.5281/zenodo.12599903.

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Heterocyclic compounds are gaining attention for their medical and biological applications, with over 90% of new drugs containing them. Among all the heterocyclic molecules, mimics of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated. Many new nitrogen-based heterocycles have been designed. The n

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14

K. Slman, Dhuha, Hind A. Satar, Zahraa A. Ketan, and Asmaa A. Jawad. "Heterocyclic Compounds: A Study of its Biological Activity." Al-Nahrain Journal of Science 27, no. 5 (2024): 19–24. https://doi.org/10.22401/anjs.27.5.03.

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Heterocyclic compounds have gained a lot of attention because of their numerous significant medical and biological uses. Research interest on heterocyclic compounds is rapidly increasing due to the extensive synthetic study and functional utility. Heterocycles also play a role in different fields, inclusive of medicinal chemistry, biochemistry, and others. Pharmaceuticals, agrochemicals, and veterinary items are the main applications of heterocyclic compounds. In our review, we cover the majority of bio-active heterocycles that have recently been synthesized and introduced a new phase of possi

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15

Yadav, Shailendra, Sushma Singh, and Chitrasen Gupta. "A CONCISE OVERVIEW ON HETEROCYCLIC COMPOUNDS EXHIBITING PESTICIDAL ACTIVITIES." International Journal of Advanced Research 9, no. 08 (2021): 989–1004. http://dx.doi.org/10.21474/ijar01/13352.

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Heterocyclic compounds are numerous and diverse group of organic compounds. Heterocycles are abundantly found in nature and express various physiological properties. Heterocycles are intricately linked to all aspects of life. There are many heterocyclic compounds currently known, and the number is constantly rising owing to extensive synthetic development and their applications. Heterocyclic compounds are used significantly in a number of areas, including biochemistry and medicinal chemistry, and some others. They are predominantly synthesized in agrochemical and pharmaceutical industries due

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16

Maji, Pradip Kumar. "Recent Progress in the Synthesis of Pyrimidine Heterocycles: A Review." Current Organic Chemistry 24, no. 10 (2020): 1055–96. http://dx.doi.org/10.2174/1385272824999200507123843.

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Pyrimidine heterocycles are proven to be biologically active heterocycles, found in many biological systems, displaying a broad spectrum of biological activities including anticancer, anxiolytic, antioxidant, antiviral, antifungal, anticonvulsant, antidepressant and antibacterial activities. Recently, various synthetic approaches, synthetic strategy, the variation of substrates and study devoted towards the evaluation of biological activities for the pyrimidine heterocycles have been reported in the literature. This review article describes the synthesis of various biologically interesting pyr

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17

Egbujor, Melford C., Paolo Tucci, Ugomma C. Onyeije, Chigbundu N. Emeruwa, and Luciano Saso. "NRF2 Activation by Nitrogen Heterocycles: A Review." Molecules 28, no. 6 (2023): 2751. http://dx.doi.org/10.3390/molecules28062751.

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Several nitrogen heterocyclic analogues have been applied to clinical practice, and about 75% of drugs approved by the FDA contain at least a heterocyclic moiety. Thus, nitrogen heterocycles are beneficial scaffolds that occupy a central position in the development of new drugs. The fact that certain nitrogen heterocyclic compounds significantly activate the NRF2/ARE signaling pathway and upregulate the expression of NRF2-dependent genes, especially HO-1 and NQO1, underscores the need to study the roles and pharmacological effects of N-based heterocyclic moieties in NRF2 activation. Furthermor

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18

Shaikh, Ansar R., Mazahar Farooqui, R. H. Satpute, and Syed Abed. "Overview on Nitrogen containing compounds and their assessment based on ‘International Regulatory Standards’." Journal of Drug Delivery and Therapeutics 8, no. 6-s (2018): 424–28. http://dx.doi.org/10.22270/jddt.v8i6-s.2156.

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Heterocyclic compounds have a role in most fields of sciences such as medicinal chemistry, biochemistry also another area of sciences. More than 90% of new drugscontain heterocycles and the interface between chemistry and biology, at which so much new scientific insight, discovery and application is taking place is crossed by heterocyclic compounds. Compounds derived from heterocyclic rings in pharmacy, medicine, agriculture, plastic, polymer and other fields.Most active heterocycles that have shown considerable biological actions as antifungal, anti-inflammatory, antibacterial, anticonvulsant

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19

Dudhe, Anshu R., Sachinkumar D. Gunjal, Sampath AG, Sushama Rawat, and YY Nandurkar. "An Overview on Nitrogen-containing Heterocyclic Compounds as Anticancer Agents." INTERNATIONAL JOURNAL OF PHARMACEUTICAL QUALITY ASSURANCE 14, no. 04 (2023): 1296–301. http://dx.doi.org/10.25258/ijpqa.14.4.72.

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Cancer accounts for nearly 10 million losses each year. Among the most prevalent cancer types are breast, lung, colon, rectum, and prostate cancers. Astonishingly, around one-third of cancer-related deaths can be attributed to factors such as tobacco usage, a high body mass index (BMI), alcohol consumption, restricted ingestion of fruits and vegetables, and inadequate bodily bustle. In the field of pharmaceuticals, heteroatoms and heterocyclic compounds frequently assume crucial roles and serve as common structural components in numerous active natural products. Statistically, the majority of

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20

Niedballa, Jonas, and Thomas J. J. Müller. "Heterocycles by Consecutive Multicomponent Syntheses via Catalytically Generated Alkynoyl Intermediates." Catalysts 12, no. 1 (2022): 90. http://dx.doi.org/10.3390/catal12010090.

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Multicomponent processes are beneficial tools for the synthesis of heterocycles. As densely substituted bifunctional electrophiles, ynones are essential intermediates by applying cyclocondensations or cycloadditions in numerous heterocycle syntheses. The respective alkynoyl intermediates are generally accessible by palladium-, copper- and palladium/copper-catalyzed alkynylation. In turn, the mild reaction conditions allow for a fast and versatile entry to functional heterocycles in the sense of consecutive multicomponent processes. This review collates and presents recent advances in accessing

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21

Drapak, І. V. "In silico screening of drug-like molecules for the treatment of cardiovascular diseases on the basis of five-membered privileged heterocycles." Farmatsevtychnyi zhurnal, no. 4 (September 10, 2019): 61–72. http://dx.doi.org/10.32352/0367-3057.4.19.07.

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Among various heterocyclic systems, the derivatives of five-membered heterocycles are of special interest. Most of the above mentioned heterocycles are treatred as so-called privileged structures in modern medicinal chemistry. In silico screening among five-membered heterocycles of molecules for the treatment of cardiovascular diseases is actual. The aim of the work was the search for synthetic drug-like molecules based on functionalized five-membered heterocycles and related heterocyclic systems as an element of the theoretical platform for rational design of compounds acting on the car

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22

Birzan, Liviu, Mihaela Cristea, Constantin C. Draghici, and Alexandru C. Razus. "Some Considerations Regarding the 1H and 13C Spectra of 4-(1-azulenyl)-2,6-bis(2-heteroaryl-vinyl)- pyrylium and Pyridinium and their Corresponding Pyridines." Revista de Chimie 69, no. 1 (2018): 64–69. http://dx.doi.org/10.37358/rc.18.1.6045.

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The 1H and 13C NMR spectra of several 2,6-diheteroarylvinyl heterocycles containing 4-azulenyl moiety were recorded and their proton and carbon chemical shifts were compared with those of the compounds without double bond between the heterocycles. The influence of the nature of central and side heterocycles, molecule polarization and anisotropic effects were revealed. The highest chemical shifts were recorded for the pyrylium salts and the lowest at pyridines, but in the case of the pyridinium salts, the protons chemical shifts at the central heterocycle are more shielded due to a peculiar ani

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23

Sharma, Deepak, Vinay Kumar, Khushboo Rani, and Vishal Ahuja. "Exploration of current advances in the anti-cancer heterocyclic compounds and their mechanism of action." INDIAN JOURNAL OF HETEROCYCLIC CHEMISTRY 35, no. 02 (2025): 223. https://doi.org/10.59467/ijhc.2025.35.223.

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The current review article presents a comprehensive information on the contribution of heterocyclic compounds (HCs) in the treatment of life-threatening disease cancer. The study highlights recent global tolls of cancer, existing therapeutic technologies, challenges with current treatment lines, and possible solutions to overcome these challenges. Review articles provide a comparative information on the classification of anti-cancer HCs and their structures. The review article also covers the anti-cancer mechanisms exhibited by the heterocycles. Furthermore, review manuscripts include the rece

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Charushin, V. N., E. V. Verbitskiy, O. N. Chupakhin, et al. "The chemistry of heterocycles in the 21st century." Russian Chemical Reviews 93, no. 7 (2024): RCR5125. http://dx.doi.org/10.59761/rcr5125.

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The chemistry of heterocyclic compounds has traditionally been and remains a bright area of chemical science in Russia. This is due to the fact that many heterocycles find the widest application. These compounds are the key structural fragments of most drugs, plant protection agents. Many natural compounds are also derivatives of heterocycles. At present, more than half of the hundreds of millions of known chemical compounds are heterocycles. This collective review is devoted to the achievements of Russian chemists in this field over the last 15–20 years. The review presents the achievements o

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25

Soloshonok, Vadim. "CARBON NANOTUBES-CATALYZED SYNTHESIS OF FLUORINE-CONTAINING HETEROCYCLES." Ukrainian Chemistry Journal 90, no. 6 (2024): 71–86. https://doi.org/10.33609/2708-129x.90.6.2024.71-86.

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Fluorine-containing heterocycles play a crucial role in modern pharmaceuticals, agrochemicals, and material sciences. The quest for effective and sustainable methods to prepare fluorinated heterocycles has led to the exploration of various nanomaterials as potential catalysts. Among these, carbon nanotubes (CNTs) have emerged as promising heterogeneous catalysts for the multicomponent synthesis of heterocycles, thanks to their unique properties. These properties include tunable surface chemistry, exceptional thermal and chemical stability, and near-complete reusability. This review aims to p

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26

Li, Jin-Heng, De-Lie An, and Jing-Hao Qin. "Recent Advances in Cycloaddition Reactions with Alkynes to Construct Heterocycles." Synthesis 52, no. 24 (2020): 3818–36. http://dx.doi.org/10.1055/s-0040-1707355.

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Heterocyclic compounds, especially N-heterocycles and O-heterocycles, are prominent structural motifs present in numerous natural products and medically and/or economically important compounds. This review aims to describe the development of transition-metal-catalyzed cycloaddition reactions of functionalized m-atom partners with alkynes to access a wide range of five-, six-, and seven-membered heterocycles, that is functionalized N-heterocycles and O-heterocycles such as azepines, isoquinolines, isocoumarins, spiroheterocycles, indoles, furans, and pyrroles, in a selectively controlled manner

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27

Sparr, Christof, and Christian Fischer. "Configurationally Stable Atropisomeric Acridinium Fluorophores." Synlett 29, no. 16 (2018): 2176–80. http://dx.doi.org/10.1055/s-0037-1610233.

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Arylated heterocyclic fluorophores are particularly useful scaffolds for numerous applications, such as bioimaging or synthetic photochemistry. While variation of the substitution pattern at the heterocycle and aryl groups allows dye modulation, the bond rotational barriers are also strongly affected. Unsymmetrically substituted ring systems of rotationally restricted arylated heterocycles therefore lead to configurationally stable atropisomeric fluorophores. Herein, we describe these characteristics by determining the properties and configurational stability of atropisomeric, tri-ortho-substi

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Adak, Laksmikanta, and Tubai Ghosh. "Recent Progress in Iron-Catalyzed Reactions Towards the Synthesis of Bioactive Five- and Six-Membered Heterocycles." Current Organic Chemistry 24, no. 22 (2020): 2634–64. http://dx.doi.org/10.2174/1385272824999200714102103.

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Heterocyclic compounds are the largely diverse organic molecules and find prevalent applications in the fine chemical industry, medicinal chemistry and agricultural science. They are also among the most commonly bearing frameworks in numerous drugs and pharmaceutical substances. Therefore, the development of convenient, efficient and environmentally benign methods to produce various types of heterocyclic compounds is an attractive area of research. For the synthesis and functionalization of heterocycles, enormous achievements have been attributed over the past decades. Recently, ironcatalyzed

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Moulis, Pierre, Cécile Miot-Sertier, Laure Cordazzo, et al. "Which microorganisms contribute to mousy off-flavour in our wines?" OENO One 57, no. 2 (2023): 177–87. http://dx.doi.org/10.20870/oeno-one.2023.57.2.7481.

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In recent years, the frequency of occurrence of mousy off-flavours in wines has increased. This could be caused by the significant decrease in sulphur dioxide addition during processing, the increase in pH or even the trend for spontaneous fermentation in wine. This off-flavour was associated with Brettanomyces bruxellensis or lactic acid bacteria metabolisms. Three N-heterocyclic compounds (APY, ETHP, ATHP) were described as involved in mousiness perception. Thus far, no study addressed the variability in that N-heterocycles production according to microorganism strains from different species

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Hoffman, Gavin R., and Allen M. Schoffstall. "Syntheses and Applications of 1,2,3-Triazole-Fused Pyrazines and Pyridazines." Molecules 27, no. 15 (2022): 4681. http://dx.doi.org/10.3390/molecules27154681.

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Pyrazines and pyridazines fused to 1,2,3-triazoles comprise a set of heterocycles obtained through a variety of synthetic routes. Two typical modes of constructing these heterocyclic ring systems are cyclizing a heterocyclic diamine with a nitrite or reacting hydrazine hydrate with dicarbonyl 1,2,3-triazoles. Several unique methods are known, particularly for the synthesis of 1,2,3-triazolo[1,5-a]pyrazines and their benzo-fused quinoxaline and quinoxalinone-containing analogs. Recent applications detail the use of these heterocycles in medicinal chemistry (c-Met inhibition or GABAA modulating

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Kerru, Nagaraju, Lalitha Gummidi, Suresh Maddila, Kranthi Kumar Gangu, and Sreekantha B. Jonnalagadda. "A Review on Recent Advances in Nitrogen-Containing Molecules and Their Biological Applications." Molecules 25, no. 8 (2020): 1909. http://dx.doi.org/10.3390/molecules25081909.

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The analogs of nitrogen-based heterocycles occupy an exclusive position as a valuable source of therapeutic agents in medicinal chemistry. More than 75% of drugs approved by the FDA and currently available in the market are nitrogen-containing heterocyclic moieties. In the forthcoming decade, a much greater share of new nitrogen-based pharmaceuticals is anticipated. Many new nitrogen-based heterocycles have been designed. The number of novel N-heterocyclic moieties with significant physiological properties and promising applications in medicinal chemistry is ever-growing. In this review, we co

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32

Kumar, Adarsh, Ankit Kumar Singh, Harshwardhan Singh, et al. "Nitrogen Containing Heterocycles as Anticancer Agents: A Medicinal Chemistry Perspective." Pharmaceuticals 16, no. 2 (2023): 299. http://dx.doi.org/10.3390/ph16020299.

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Cancer is one of the major healthcare challenges across the globe. Several anticancer drugs are available on the market but they either lack specificity or have poor safety, severe side effects, and suffer from resistance. So, there is a dire need to develop safer and target-specific anticancer drugs. More than 85% of all physiologically active pharmaceuticals are heterocycles or contain at least one heteroatom. Nitrogen heterocycles constituting the most common heterocyclic framework. In this study, we have compiled the FDA approved heterocyclic drugs with nitrogen atoms and their pharmacolog

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Nayl, AbdElAziz A., Ashraf A. Aly, Wael A. A. Arafa, et al. "Azides in the Synthesis of Various Heterocycles." Molecules 27, no. 12 (2022): 3716. http://dx.doi.org/10.3390/molecules27123716.

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In this review, we focus on some interesting and recent examples of various applications of organic azides such as their intermolecular or intramolecular, under thermal, catalyzed, or noncatalyzed reaction conditions. The aforementioned reactions in the aim to prepare basic five-, six-, organometallic heterocyclic-membered systems and/or their fused analogs. This review article also provides a report on the developed methods describing the synthesis of various heterocycles from organic azides, especially those reported in recent papers (till 2020). At the outset, this review groups the synthet

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34

Xia, Xiao-Feng, та Yan-Ning Niu. "Recent developments in the synthesis of nitrogen-containing heterocycles from β-aminovinyl esters/ketones as CC–N donors". Organic & Biomolecular Chemistry 20, № 2 (2022): 282–95. http://dx.doi.org/10.1039/d1ob01998h.

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Kaur, Navjeet. "Metal and Non-Metal Catalysts in the Synthesis of Five-Membered S-Heterocycles." Current Organic Synthesis 16, no. 2 (2019): 258–75. http://dx.doi.org/10.2174/1570179416666181207144430.

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Background:A wide variety of biological activities are exhibited by N, O and S containing heterocycles and recently, many reports appeared for the synthesis of these heterocycles. The synthesis of heterocycles with the help of metal and non-metal catalyst has become a highly rewarding and important method in organic synthesis. This review article concentrated on the synthesis of S-heterocylces in the presence of metal and non-metal catalyst. The synthesis of five-membered S-heterocycles is described here.Objective:There is a need for the development of rapid, efficient and versatile strategy f

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36

Perlmutter, Patrick. "The Nucleophilic Addition/Eiectrophilic Ring Closure Route to Bio-Active Heterocycles." Current Medicinal Chemistry 3, no. 2 (1996): 139–52. http://dx.doi.org/10.2174/092986730302220302101738.

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Abstract: Many bio-active compounds contain one or more saturated or partially saturated heterocycles. Most of these contain one or more stereo centres. As a result any attempts to synthesize these compounds must take full account of the stereochemistry. In this article a new approach to the stereoselective synthesis of heterocycles is reviewed. The emphasis is on oxygen-containing heterocycles. The approach involves a sequence of a nucleophilic addition reaction followed by an electrophilic ring closure. Examples are given of the stereoselective synthesis of the heterocyclic subunits of macr

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37

Maciejewski, Andrzej, Anna Jaworska-Augustyniak, Dariusz Radocki, Ronald G. Sutherland, and Adam Piórko. "An efficient photochemical formation of phenoxazine and phenothiazine from their respective cyclopentadienyliron complexes." Collection of Czechoslovak Chemical Communications 54, no. 8 (1989): 2171–75. http://dx.doi.org/10.1135/cccc19892171.

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The photochemical liberation of phenoxazine and phenothiazine from their cyclopentadienyliron complexes was studied in THF, methanol and dimethylsulfoxide. Quantum yields of decay of the complexes and the formation of free heterocycles have been determined to be about 1.0, independent of solvent, concentration and wavelength of light used. The ease of isolation of free heterocycles after photolysis show that this efficient way of heterocycle recovery is superior to the previously utilized pyrolytic sublimation.

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Zhu, Daqian, Zhouming Wu, Liyun Liang, et al. "Heterocyclic iodoniums as versatile synthons to approach diversified polycyclic heteroarenes." RSC Advances 9, no. 57 (2019): 33170–79. http://dx.doi.org/10.1039/c9ra07288h.

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Mohareb, Rafat, and Hanaa Hana. "Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activity." Acta Pharmaceutica 58, no. 1 (2008): 29–42. http://dx.doi.org/10.2478/v10007-007-0043-3.

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Synthesis of progesterone heterocyclic derivatives of potential antimicrobial activityThe aim of this work was to synthesize steroidal heterocycles and to elucidate the potential role of these compounds as antimicrobial agents. The synthesis of steroidal heterocycles containing the pyrazole, isoxazole, thiazole, pyrane, pyridine, pyridazine, or benzopyrane ring attached to the pregnene nucleus is reported. Progesterone (1) reacts with dimethyl formamide dimethyl acetal to form enamine2. Heterocyclization of2with hydrazines, hydroxylamine, glycine, ethyl acetoacetate or cyanomethylene afforded

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40

Munzeiwa, Wisdom A., Bernard Omondi, and Vincent O. Nyamori. "Architecture and synthesis of P,N-heterocyclic phosphine ligands." Beilstein Journal of Organic Chemistry 16 (March 12, 2020): 362–83. http://dx.doi.org/10.3762/bjoc.16.35.

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Diverse P,N-phosphine ligands reported to date have performed exceptionally well as auxiliary ligands in organometallic catalysis. Phosphines bearing 2-pyridyl moieties prominently feature in literature as compared to phosphines with five-membered N-heterocycles. This discussion seeks to paint a broad picture and consolidate different synthetic protocols and techniques for N-heterocyclic phosphine motifs. The introduction provides an account of P,N-phosphine ligands, and their structural and coordination benefits from combining heteroatoms with different basicity in one ligand. The body discus

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Geisenberger, Josef, Jürgen Erbe, Jürgen Heidrich, Ulrich Nagela, and Wolfgang Beck. "Pseudohalogenometallverbindungen, LXV [1] Synthese von Tetrazolen und Triazolen über die 1,3-dipolare Cycloaddition an die Azid-Liganden von polymeren Cobalt(III)-und Palladium(II)-Komplexen. Darstellung und Struktur von 5-TrichlormethyItetrazol / Pseudohalogeno Metal Compounds, LXV [1] Synthesis of Tetrazoles and Triazoles via 1,3-Dipolar Cycloaddition to the Azido Ligands of Polymerie Cobalt(III) and Palladium(II) Complexes. Synthesis and Structure of 5-Trichloromethyltetrazole." Zeitschrift für Naturforschung B 42, no. 1 (1987): 55–64. http://dx.doi.org/10.1515/znb-1987-0112.

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Abstract The cycloaddition of nitriles and of dimethylacetylenedicarboxylate to the azide ligand of polymeric Schiff Base cobalt(III) and phosphine palladium(II) complexes gives the corresponding tetrazolate and triazolate complexes from which the heterocycles could be cleaved by hydrogen chloride. Usually the yields are low; if the heterocycle is soluble in ether or sublimable, yields up to 30% have been obtained. Using this method the hitherto unknown 5-trichlormethyltetrazole could be prepared which was characterized by an X-ray structural analysis. Similarly, the cyclo-addition of azido(te

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42

Groso, Emilia, and Corinna Schindler. "Recent Advances in the Application of Ring-Closing Metathesis for the Synthesis of Unsaturated Nitrogen Heterocycles." Synthesis 51, no. 05 (2019): 1100–1114. http://dx.doi.org/10.1055/s-0037-1611651.

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This short review summarizes recent advances relating to the application of ring-closing olefin-olefin and carbonyl-olefin metathesis reactions towards the synthesis of unsaturated five- and six-membered nitrogen heterocycles. These developments include catalyst modifications and reaction designs that will enable access to more complex nitrogen heterocycles.1 Introduction2 Expansion of Ring-Closing Metathesis Methods3 Evaluation of Catalyst Design4 Indenylidene Catalysts5 Unsymmetrical N-Heterocyclic Carbene Ligands6 Carbonyl-Olefin Metathesis7 Conclusions

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Huang, Pengfei, Pan Wang, Shengchun Wang, Shan Tang, and Aiwen Lei. "Electrochemical oxidative [4 + 2] annulation of tertiary anilines and alkenes for the synthesis of tetrahydroquinolines." Green Chemistry 20, no. 21 (2018): 4870–74. http://dx.doi.org/10.1039/c8gc02463d.

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Yuan, Dan, Ziting Xu, Yang Zhou, et al. "Palladium-Catalyzed Cascade Reactions for Synthesis of Heterocycles Initiated by C(sp3)–H Functionalization." Catalysts 15, no. 1 (2025): 72. https://doi.org/10.3390/catal15010072.

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Heterocycles are widely present in natural products, pharmaceuticals, and organic functional materials. In heterocycle synthesis, Pd-catalyzed cascade C–H functionalization has been regarded as one of the most powerful approaches due to its advantages in terms of high atom efficiency and readily available starting materials. In this review, we will briefly introduce the major advances in palladium-catalyzed cascade C(sp3)–H activation and annulation for constructing different types of heterocycles through inter- and intramolecular pathways from 2010 to 2023.

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Breitwieser, Kevin, and Peter Chen. "Crystal structure of a 1,1-dibutyl-1H,3H-naphtho[1,8-cd][1,2,6]oxastannaborinin-3-ol." Acta Crystallographica Section E Crystallographic Communications 77, no. 2 (2021): 180–83. http://dx.doi.org/10.1107/s2056989021000712.

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The title oxastannaborininol compound, [Sn(C4H9)2(C10H7BO2)], has been synthesized and crystallized. While heterocycles containing a C–O–B group are common, heterocycles containing an E–O–B unit, where E is an element of the carbon group except for carbon, are rare. In fact, while heterocycles containing Si–O–B units are occasionally reported (although without crystal structures), there are no reports for the corresponding germanium, tin or lead analogues. Herein, the first synthesis and crystal structure of a heterocycle containing an Sn–O–B unit is described. The asymmetric unit contains one

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Shi, Jueying, Miao Yu, Weikang Chen, et al. "Recent Discovery of Nitrogen Heterocycles from Marine-Derived Aspergillus Species." Marine Drugs 22, no. 7 (2024): 321. http://dx.doi.org/10.3390/md22070321.

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Nitrogen heterocycles have drawn considerable attention because of their structurally novel and significant biological activities. Marine-derived fungi, especially the Aspergillus species, possess unique metabolic pathways to produce secondary metabolites with novel structures and potent biological activities. This review prioritizes the structural diversity and biological activities of nitrogen heterocycles that are produced by marine-derived Aspergillus species from January 2019 to January 2024, and their relevant biological activities. A total of 306 new nitrogen heterocycles, including sev

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Boelke, Andreas, Soleicha Sadat, Enno Lork, and Boris J. Nachtsheim. "Pseudocyclic bis-N-heterocycle-stabilized iodanes – synthesis, characterization and applications." Chemical Communications 57, no. 60 (2021): 7434–37. http://dx.doi.org/10.1039/d1cc03097c.

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Li, Xianwei, Tianzhang Wang, Yu-Jing Lu, Shaomin Ji, Yanping Huo, and Bifu Liu. "Copper-catalyzed oxidative multicomponent reaction: synthesis of imidazo fused heterocycles with molecular oxygen." Organic & Biomolecular Chemistry 16, no. 39 (2018): 7143–51. http://dx.doi.org/10.1039/c8ob01532e.

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An oxidative cascade that involves multicomponent reaction comprising a terminal alkyne, 2-amino N-heterocycle, benzyl or allylic bromide with molecular oxygen, delivering densely functionalized imidazo fused heterocycles, is achieved.

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49

DeCicco, Ethan M., Neively Tlapale-Lara, and Shauna M. Paradine. "Incorporating azaheterocycle functionality in intramolecular aerobic, copper-catalyzed aminooxygenation of alkenes." RSC Advances 14, no. 39 (2024): 28822–26. http://dx.doi.org/10.1039/d4ra06178k.

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A key limitation across aminofunctionalizations is incompatibility with substrates bearing medicinally relevant N-heterocycles; in contrast, this aerobic, Cu-catalyzed aminooxygenation engages a diverse range of N-heterocycle-bearing substrates.

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50

Castagnolo, Daniele, Fei Zhao, Domiziana Masci, and Elena Tomarelli. "Biocatalytic and Chemo-Enzymatic Approaches for the Synthesis of Heterocycles." Synthesis, July 28, 2020. http://dx.doi.org/10.1055/s-0040-1707210.

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Heterocycles are ubiquitous structures in nature and can be found in many drugs and chemicals. Biocatalysts, alone or in combination with other metal catalysts, can be exploited for the construction of various heterocyclic rings under mild reaction conditions. This Short Review highlights the recent advances in the development of biocatalytic and chemo-enzymatic methods for the synthesis of both aliphatic and aromatic heterocyclic rings.1 Introduction2 Synthesis of Aliphatic Heterocycles2.1 Piperidines, Pyrrolidines and Piperazines2.2 Other Nitrogen-Containing Aliphatic Heterocycles2.3 Lactone

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