scholarly journals An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles

2013 ◽  
Vol 9 ◽  
pp. 2265-2319 ◽  
Author(s):  
Marcus Baumann ◽  
Ian R Baxendale
Keyword(s):  
Pharmaceutical Compounds ◽  
Heterocyclic Ring ◽  
Reference Source ◽  
Scientific Journals ◽  
Drug Molecules ◽  
Patent Literature ◽  
Synthetic Routes

This review which is the second in this series summarises the most common synthetic routes as applied to the preparation of many modern pharmaceutical compounds categorised as containing a six-membered heterocyclic ring. The reported examples are based on the top retailing drug molecules combining synthetic information from both scientific journals and the wider patent literature. It is hoped that this compilation, in combination with the previously published review on five-membered rings, will form a comprehensive foundation and reference source for individuals interested in medicinal, synthetic and preparative chemistry.

Synthetic routes to benzosuberone-based fused- and spiro-heterocyclic ring systems

RSC Advances ◽  
2016 ◽  
Vol 6 (22) ◽  
pp. 17955-17979 ◽  
Author(s):  
Thoraya A. Farghaly ◽  
Sobhi M. Gomha ◽  
Kamal M. Dawood ◽  
Mohamed R. Shaaban
Keyword(s):  
Pharmaceutical Compounds ◽  
Heterocyclic Ring ◽  
Present Review ◽  
Important Class ◽  
Ring Systems ◽  
Synthetic Routes

Benzosuberones are an important class of medicinal and pharmaceutical compounds and have recently attracted considerable attention. The present review highlights the progress in the synthesis of benzosuberones and their fused and spiro ring systems up to 2015.

scholarly journals An overview of the key routes to the best selling 5-membered ring heterocyclic pharmaceuticals

2011 ◽  
Vol 7 ◽  
pp. 442-495 ◽  
Author(s):  
Marcus Baumann ◽  
Ian R Baxendale ◽  
Steven V Ley ◽  
Nikzad Nikbin
Keyword(s):  
Membered Ring ◽  
Comprehensive Overview ◽  
Vast Number ◽  
Drug Compounds ◽  
Patent Literature ◽  
Synthetic Routes

This review presents a comprehensive overview on selected synthetic routes towards commercial drug compounds as published in both journal and patent literature. Owing to the vast number of potential structures, we have concentrated only on those drugs containing five-membered heterocycles and focused principally on the assembly of the heterocyclic core. In order to target the most representative chemical entities the examples discussed have been selected from the top 200 best selling drugs of recent years.

ChemInform Abstract: Synthetic Routes to Benzosuberone-Based Fused- and Spiro-Heterocyclic Ring Systems

ChemInform ◽  
2016 ◽  
Vol 47 (15) ◽  
pp. no-no
Author(s):  
Thoraya A. Farghaly ◽  
Sobhi M. Gomha ◽  
Kamal M. Dawood ◽  
Mohamed R. Shaaban
Keyword(s):  
Heterocyclic Ring ◽  
Ring Systems ◽  
Synthetic Routes

Methods of Synthesis of Remdesivir, Favipiravir, Hydroxychloroquine, and Chloroquine: Four Small Molecules Repurposed for Clinical Trials during the Covid-19 Pandemic

Synthesis ◽  
2020 ◽  
Vol 52 (24) ◽  
pp. 3735-3750 ◽  
Author(s):  
Nader Al Bujuq
Keyword(s):  
Small Molecules ◽  
New Drugs ◽  
Reference Source ◽  
The Novel ◽  
Efficacy And Safety ◽  
Health Measures ◽  
Drug Molecules ◽  
Agency Support ◽  
Methods Of Synthesis ◽  
Novel Coronavirus

AbstractThe novel coronavirus (COVID-19) disease has rapidly evolved into a sweeping pandemic despite public health measures. Screening and development of new vaccines and antivirals are expensive and time consuming. However, the repositioning of available drugs is an essential and universal strategy in the development of new drugs and therefore should receive priority attention as well as international government and agency support. Significant drugs such as chloroquine, hydroxychloroquine, favipiravir and remdesivir, are currently undergoing clinical studies to test their efficacy and safety. Some promising results have been achieved thus far in the treatment of COVID-19. In this article we summarize and discuss the most common synthetic strategies to apply in the preparation of these drug molecules. It is hoped that this compendium will provide an accessible useful guide and reference source for scientists, researchers and academia in their battle against COVD-19.1 Introduction2 Synthesis of Chloroquine (CQ) and Hydroxychloroquine (HCQ)2.1 Synthesis of 4,7-Dichloroquinoline 1 2.2 Synthesis of 2-Amino-5-(diethylamino)pentane (Novoldiamine) 2 2.3 Synthesis of 5-(N-Ethyl-N-2-hydroxyethylamino)-2-pentylamine 4 2.4 Developed Methods for Synthesis of Chloroquine and Hydroxychloroquine2.5 Synthesis of (R)-Chloroquine, (S)-Chloroquine, (R)-Hydroxychloroquine and (S)-Hydroxychloroquine3 Synthesis of Favipiravir (Avigan)4 Synthesis of Remdesivir5 Conclusion

scholarly journals Current Updates on Oxazolidinone and Its Significance

2012 ◽  
Vol 2012 ◽  
pp. 1-24 ◽  
Author(s):  
Neha Pandit ◽  
Rajeev K. Singla ◽  
Birendra Shrivastava
Keyword(s):  
Antibacterial Activity ◽  
Mechanism Of Action ◽  
Heterocyclic Ring ◽  
Pharmacological Mechanism ◽  
Research Activities ◽  
Current Review ◽  
Review Articles ◽  
Medicinal Properties ◽  
Synthetic Routes ◽  
Heterocyclic Structure

Oxazolidinone is a five-member heterocyclic ring exhibiting potential medicinal properties with preferential antibacterial activity. Scientists reported various synthetic procedures for this heterocyclic structure. Current review articles tried to cover each and every potential aspect of oxazolidinone like synthetic routes, pharmacological mechanism of action, medicinal properties, and current research activities.

scholarly journals Features of the synthesis and biological evaluation of 3-(carboxyphenyl)chromones

2020 ◽  
Vol 15 (2) ◽  
pp. 3-12
Author(s):  
Olga Shablykina ◽  
Viktoriia Moskvina ◽  
Volodymyr Khilya
Keyword(s):  
Biological Activity ◽  
Biological Evaluation ◽  
Therapeutic Agents ◽  
New Drugs ◽  
Pharmacological Activities ◽  
Chromone Derivatives ◽  
Methods Of Synthesis ◽  
Patent Literature ◽  
Synthetic Routes ◽  
Synthesis And Biological Evaluation

Flavonoids and their derivatives have historically been a source of therapeutic agents. Every year, more and more data is published on new flavonoid compounds, both synthetic and isolated from natural sources, and their innumerable physiological and pharmacological activities. This review presents synthetic routes towards 3-(carboxyphenyl)chromones and evaluation of their biological activity as published in both journal and patent literature. We have focused specifically on the 3-(carboxyphenyl)chromones, because while methods of synthesis and biological activity of 2(3)-substituted and 2,3-disubstituted chromones are well studied, literature data on isoflavones containing a carboxyl, ester, or amide group in ring B is scarce and fragmentary. The presented generalization of synthetic strategies and biological activity of 3-(carboxyphenyl)chromone derivatives demonstrates that this class of compounds can be targeted for discovery of new drugs and can be readily prepared owing to recent advances in synthetic organic and medicinal chemistry.

The construction of benzimidazo[2,1-a]isoquinolin-6(5H)-ones from N-methacryloyl-2-phenylbenzoimidazoles through radical strategies

2021 ◽  
Author(s):  
Qing-Qing Kang ◽  
Wei-Kang Zhang ◽  
Guo-Ping Ge ◽  
Hongxing Zheng ◽  
Wenting Wei
Keyword(s):  
Natural Products ◽  
Functional Materials ◽  
Pharmaceutical Compounds ◽  
Biologically Active ◽  
Synthetic Routes ◽  
Active Natural

Benzimidazo[2,1-a]isoquinolin-6(5H)-one constitute a structurally unique class of tetracyclic N-heterocycles that are found throughout myriad biologically active natural products, pharmaceutical compounds, and functional materials. Various synthetic routes for the preparation of...

Total synthesis of biologically active alkaloids using transition metals

2010 ◽  
Vol 82 (11) ◽  
pp. 1975-1991 ◽  
Author(s):  
Ronny Forke ◽  
Konstanze K. Gruner ◽  
Kerstin E. Knott ◽  
Stefan Auschill ◽  
Sameer Agarwal ◽  
...  
Keyword(s):  
Transition Metals ◽  
Total Synthesis ◽  
Binding Site ◽  
Heterocyclic Ring ◽  
Myosin Atpase ◽  
Biologically Active ◽  
Ring Systems ◽  
Atpase Inhibitors ◽  
Synthetic Routes ◽  
Carbazole Alkaloids

We have developed efficient synthetic routes to heterocyclic ring systems using transition metals (palladium, iron, and silver). Recent applications of this chemistry to the total synthesis of biologically active alkaloids include carbazole alkaloids (pityriazole, euchrestifoline, the antiostatins), crispine A, pentabromo- and pentachloropseudilin. The two latter alkaloids represent a novel class of myosin ATPase inhibitors that led to the discovery of a new allosteric binding site of the protein.

Formylation of carbohydrates and the evolution of synthetic routes to artificial oligosaccharides and glycoconjugates

2000 ◽  
Vol 72 (9) ◽  
pp. 1577-1588 ◽  
Author(s):  
Alessandro Dondoni
Keyword(s):  
Amino Acid ◽  
Heterocyclic Ring ◽  
Synthetic Methods ◽  
Formyl Group ◽  
Alternative Synthesis ◽  
Synthetic Utility ◽  
Highly Effective ◽  
Synthetic Routes ◽  
Galactosyl Ceramide

A highly effective method for the synthesis of formyl C-glycosides is described via addition of 2-lithiothiazole or 2-lithiobenzothiazole to sugar lactones, deoxygenation of the resulting ketols, and releasing of the formyl group from the heterocyclic ring. The synthetic utility of these sugar aldehydes is demonstrated by the development of synthetic methods to more elaborate C-glycosides. These include various (1-6)-C-disaccharides and some higher oligomers up to a C,C,C,C-pentasaccharide; C-glycosyl amino acid isosteres of N-glycosyl asparagines; the methylene isostere of β-Δ-galactosyl ceramide; linear and cylic (2-1)-ketoside oligomers. An alternative synthesis of ethylene-bridged glycosyl asparagine isosteres is illustrated by the use of ethynyl C-glycosides as starting materials.

scholarly journals Critical Assessment of Streptomyces spp. Able to Control Toxigenic Fusaria in Cereals: A Literature and Patent Review

2019 ◽  
Vol 20 (24) ◽  
pp. 6119 ◽  
Author(s):  
Elena Maria Colombo ◽  
Andrea Kunova ◽  
Paolo Cortesi ◽  
Marco Saracchi ◽  
Matias Pasquali
Keyword(s):  
Fusarium Species ◽  
Toxin Production ◽  
Genus Streptomyces ◽  
Toxigenic Fungi ◽  
Drug Molecules ◽  
Streptomyces Spp ◽  
Disease Occurrence ◽  
Patent Review ◽  
Patent Literature ◽  
Year 2000

Mycotoxins produced by Fusarium species on cereals represent a major concern for food safety worldwide. Fusarium toxins that are currently under regulation for their content in food include trichothecenes, fumonisins, and zearalenone. Biological control of Fusarium spp. has been widely explored with the aim of limiting disease occurrence, but few efforts have focused so far on limiting toxin accumulation in grains. The bacterial genus Streptomyces is responsible for the production of numerous drug molecules and represents a huge resource for the discovery of new molecules. Streptomyces spp. are also efficient plant colonizers and able to employ different mechanisms of control against toxigenic fungi on cereals. This review describes the outcomes of research using Streptomyces strains and/or their derived molecules to limit toxin production and/or contamination of Fusarium species in cereals. Both the scientific and patent literature were analyzed, starting from the year 2000, and we highlight promising results as well as the current pitfalls and limitations of this approach.

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