Halogenated Heterocycles for Drug Discovery

Halogenated Heterocycles for Drug Discovery PDF Author: Ian Wilson
Publisher:
ISBN:
Category : Heterocyclic compounds
Languages : en
Pages :

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Book Description
Within a number of industries, and particularly within the pharmaceutical industry, there is a desire for reliable, high yielding routes towards large numbers of valuable small molecules that allow a wide range of products to be synthesised. Heterocyclic compounds are particularly sought after as useful compounds, with an estimated 70% of pharmaceutical products being based on heterocyclic structures. A drawback of many traditional routes towards heterocyclic compounds is that the range of substituents that may be placed around the ring is limited. This is especially limiting if ring substituents have to be placed early in a synthesis, reducing the opportunities for elaboration at a late stage. Our approach is to take highly halogenated heterocyclic systems and use them as scaffolds for the synthesis of novel compounds by the sequential replacement of halogen atoms with other functionalities. This approach has led to the generation of a number of novel highly substituted heterocyclic species.

Halogenated Heterocycles for Drug Discovery

Halogenated Heterocycles for Drug Discovery PDF Author: Ian Wilson
Publisher:
ISBN:
Category : Heterocyclic compounds
Languages : en
Pages :

Get Book Here

Book Description
Within a number of industries, and particularly within the pharmaceutical industry, there is a desire for reliable, high yielding routes towards large numbers of valuable small molecules that allow a wide range of products to be synthesised. Heterocyclic compounds are particularly sought after as useful compounds, with an estimated 70% of pharmaceutical products being based on heterocyclic structures. A drawback of many traditional routes towards heterocyclic compounds is that the range of substituents that may be placed around the ring is limited. This is especially limiting if ring substituents have to be placed early in a synthesis, reducing the opportunities for elaboration at a late stage. Our approach is to take highly halogenated heterocyclic systems and use them as scaffolds for the synthesis of novel compounds by the sequential replacement of halogen atoms with other functionalities. This approach has led to the generation of a number of novel highly substituted heterocyclic species.

Halogenated Heterocycles

Halogenated Heterocycles PDF Author: Jernej Iskra
Publisher: Springer Science & Business Media
ISBN: 364225103X
Category : Science
Languages : en
Pages : 326

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Book Description
G. Sandford: Perfluoroheteroaromatic Chemistry: Multifunctional Systems from Perfluorinated Heterocycles by Nucleophilic Aromatic Substitution Processes.- A. A. Gakh: Monofluorinated Heterocycles.- R. Dembinski ∙ Y. Li ∙ D. Gundapuneni ∙ A. Decker: Synthesis of beta-Halofurans.- Y. Shermolovich ∙ S. Pazenok: Synthesis of halogenated 5- and 6-membered sulfur- and Sulfur, Nitrogen Containing Heterocycles.- S. Minakata ∙ Y. Takeda ∙ J. Hayakawa: Heterocyclic Reagents Containing Nitrogen-Halogen Bond: Recent Applications.- Michael Schnürch: Recent Progress on the Halogen Dance Reaction on Heterocycles.- T. Kosjek ∙ E. Heath: Halogenated Heterocycles as Pharmaceuticals.- E. Heath ∙ T. Kosjek: Sources, Occurrence and Fate of Halogenated Heterocyclic Pharmaceuticals in the Environment.- J. Iskra: Green Methods in Halogenation of Heterocycles.

Heterocyclic Chemistry in Drug Discovery

Heterocyclic Chemistry in Drug Discovery PDF Author: Jie Jack Li
Publisher: John Wiley & Sons
ISBN: 1118354435
Category : Science
Languages : en
Pages : 688

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Book Description
Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.

Halogenated Heterocycles

Halogenated Heterocycles PDF Author: Jernej Iskra
Publisher: Springer Science & Business Media
ISBN: 3642251021
Category : Medical
Languages : en
Pages : 326

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Book Description
This book explores topics in Heterocyclic chemistry, including Perfluoroheteroaromatic Chemistry; Monofluorinated Heterocycles; Synthesis of beta-Halofurans; Halogenated Heterocycles as Pharmaceuticals; Green Methods in Halogenation of Heterocycles and more.

Heterocyclic N-Oxides

Heterocyclic N-Oxides PDF Author: Oleg V. Larionov
Publisher: Springer
ISBN: 3319606875
Category : Science
Languages : en
Pages : 163

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Book Description
The series Topics in Heterocyclic Chemistry presents critical reviews on present and future trends in the research of heterocyclic compounds. Overall the scope is to cover topics dealing with all areas within heterocyclic chemistry, both experimental and theoretical, of interest to the general heterocyclic chemistry community. The series consists of topic related volumes edited by renowned editors with contributions of experts in the field. All chapters from Topics in Heterocyclic Chemistry are published Online First with an individual DOI. In references, Topics in Heterocyclic Chemistry is abbreviated as Top Heterocycl Chem and cited as a journal.

Privileged Scaffolds in Medicinal Chemistry

Privileged Scaffolds in Medicinal Chemistry PDF Author: Stefan Bräse
Publisher: Royal Society of Chemistry
ISBN: 1782620303
Category : Medical
Languages : en
Pages : 486

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Book Description
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Indole Ring Synthesis

Indole Ring Synthesis PDF Author: Gordon W. Gribble
Publisher: John Wiley & Sons
ISBN: 0470512180
Category : Science
Languages : en
Pages : 704

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Book Description
Of the myriad of heterocycles known to man, the indole ring stands foremost for its remarkably versatile chemistry, its enormous range of biological activities, and its ubiquity in the terrestrial and marine environments. The indole ring continues to be discovered in natural products and to be employed in man-made pharmaceuticals and other materials. Given the enormous resurgence in indole ring synthesis over the past decade — highlighted by the power of transition metal catalysis — this authoritative guide addresses the need for a comprehensive presentation of the myriad of methods for constructing the indole ring, from the ancient to the modern, and from the obscure to the well-known. Following presentation of the classic indole ring syntheses and many newer methods, coverage continues with indole ring syntheses via pyrroles, indolines, oxindoles, isatins, radical and photochemical reactions, aryne cycloadditions. This extensive volume concludes with the modern transition metal–catalyzed indole ring syntheses that utilize copper, palladium, rhodium, gold, ruthenium, platinum, and other metals to fashion the indole ring Indole Ring Synthesis is a comprehensive, authoritative and up-to-date guide to the synthesis of this important heterocycle for organic chemists, pharmaceutical researchers and those interested in the chemistry of natural products.

Advances in Heterocyclic Chemistry

Advances in Heterocyclic Chemistry PDF Author:
Publisher: Academic Press
ISBN: 0128028742
Category : Science
Languages : en
Pages : 387

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Book Description
Advances in Heterocyclic Chemistry is the definitive series in the field—one of great importance to organic chemists, polymer chemists, and many biological scientists. Because biology and organic chemistry increasingly intersect, the associated nomenclature also is being used more frequently in explanations. Written by established authorities in the field from around the world, this comprehensive review combines descriptive synthetic chemistry and mechanistic insight to yield an understanding of how chemistry drives the preparation and useful properties of heterocyclic compounds. - Considered the definitive serial in the field of heterocyclic chemistry - Serves as the go-to reference for organic chemists, polymer chemists, and many biological scientists - Provides the latest comprehensive reviews written by established authorities in the field - Combines descriptive synthetic chemistry and mechanistic insight to enhance understanding of how chemistry drives the preparation and useful properties of heterocyclic compounds

Halogen Bonding in Solution

Halogen Bonding in Solution PDF Author: Stefan Huber
Publisher: John Wiley & Sons
ISBN: 3527347313
Category : Technology & Engineering
Languages : en
Pages : 418

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Book Description
Long-awaited on the importance of halogen bonding in solution, demonstrating the specific advantages in various fields - from synthesis and catalysis to biochemistry and electrochemistry! Halogen bonding (XB) describes the interaction between an electron donor and the electrophilic region of a halogen atom. Its applicability for molecular recognition processes long remained unappreciated and has mostly been studied in solid state until recently. As most physiological processes and chemical reactions take place in solution, investigations in solutions are of highest relevance for its use in organic synthesis and catalysis, pharmaceutical chemistry and drug design, electrochemistry, as well as material synthesis. Halogen Bonding in Solution gives a concise overview of halogen bond interactions in solution. It discusses the history and electronic origin of halogen bonding and summarizes all relevant examples of its application in organocatalysis. It describes the use of molecular iodine in catalysis and industrial applications, as well as recent developments in anion transport and binding. Hot topic: Halogen bonding is an important interaction between molecules or within a molecule. The field has developed considerably in recent years, with numerous different approaches and applications having been published. Unique: There are several books on halogen bonding in solid state available, but this will be the first one focused on halogen bonding in solution. Multi-disciplinary: Summarizes the history and nature of halogen bonding in solution as well as applications in catalysis, anion recognition, biochemistry, and electrochemistry. Aimed at facilitating exciting future developments in the field, Halogen Bonding in Solution is a valuable source of information for researchers and professionals working in the field of supramolecular chemistry, catalysis, biochemistry, drug design, and electrochemistry.

Synthetic Methods in Drug Discovery

Synthetic Methods in Drug Discovery PDF Author: David C. Blakemore
Publisher: Royal Society of Chemistry
ISBN: 1849738033
Category : Medical
Languages : en
Pages : 474

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Book Description
The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.