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Flow Chemistry in Drug Discovery by Jesus Alcazar,Antonio de la Hoz,Angel Díaz-Ortiz Pdf
This book reviews the challenges and opportunities posed by flow chemistry in drug discovery, and offers a handy reference tool for medicinal chemists interested in the synthesis of biologically active compounds. Prepared by expert contributors, the respective chapters cover not only fundamental methodologies and reactions, such as the application of catalysis, especially biocatalysis and organocatalysis; and non-conventional activation techniques, from photochemistry to electrochemistry; but also the development of new process windows, processes and reactions in drug synthesis. Particular attention is given to automatization and library synthesis, which are of great importance in the pharmaceutical industry. Readers will also find coverage on selected topics of general interest, such as how flow chemistry is contributing to drug discovery R&D in developing countries, and the green character of this enabling technology, for example in the production of raw materials for the pharmaceutical industry from waste. Given its scope, the book appeals to medicinal chemistry researchers working in academia and industry alike, as well as professionals involved in scale-up and drug development.
Flow Chemistry in Drug Discovery by Jesus Alcazar,Antonio de la Hoz,Angel Díaz-Ortiz Pdf
This book reviews the challenges and opportunities posed by flow chemistry in drug discovery, and offers a handy reference tool for medicinal chemists interested in the synthesis of biologically active compounds. Prepared by expert contributors, the respective chapters cover not only fundamental methodologies and reactions, such as the application of catalysis, especially biocatalysis and organocatalysis; and non-conventional activation techniques, from photochemistry to electrochemistry; but also the development of new process windows, processes and reactions in drug synthesis. Particular attention is given to automatization and library synthesis, which are of great importance in the pharmaceutical industry. Readers will also find coverage on selected topics of general interest, such as how flow chemistry is contributing to drug discovery R&D in developing countries, and the green character of this enabling technology, for example in the production of raw materials for the pharmaceutical industry from waste. Given its scope, the book appeals to medicinal chemistry researchers working in academia and industry alike, as well as professionals involved in scale-up and drug development.
Flow and Microreactor Technology in Medicinal Chemistry by Esther Alza Pdf
Learn to master a powerful technology to enable a faster drug discovery workflow The ultimate dream for medicinal chemists is the ability to synthesize new drug-like compounds with the push of a button. The key to synthesizing chemical compounds more quickly and accurately lies in computer-controlled technologies that can be optimized by machine learning. Recent developments in computer-controlled automated syntheses that rely on miniature flow reactors—with integrated analysis of the resulting products—provide a workable technology for synthesizing new chemical substances very quickly and with minimal effort. In Flow and Microreactor Technology in Medicinal Chemistry, early adopters of this ground-breaking technology describe its current and potential uses in medicinal chemistry. Based on successful examples of the use of flow and microreactor synthesis for drug-like compounds, the book introduces current as well as emerging uses for automated synthesis in a drug discovery context. Flow and Microreactor Technology in Medicinal Chemistry readers will also find: Numerous case studies that address the most common applications of this technology in the day-to-day work of medicinal chemists How to integrate flow synthesis with drug discovery How to perform enantioselective reactions under continuous flow conditions Flow and Microreactor Technology in Medicinal Chemistry is a valuable practical reference for medicinal chemists, organic chemists, and natural products chemists, whether they are working in academia or in the pharmaceutical industry.
Author : Elizabeth Farrant Publisher : Royal Society of Chemistry Page : 176 pages File Size : 47,9 Mb Release : 2011-10-04 Category : Medical ISBN : 9781849733052
New Synthetic Technologies in Medicinal Chemistry by Elizabeth Farrant Pdf
The modern synthetic chemist applies all the tools available to identify the drug-like molecules with the best chances of becoming novel drugs. This book will act as a primer for graduates and postgraduates interested in a career in drug discovery. It covers both synthetic technologies currently impacting medicinal chemistry and emerging areas. The chapters focus on topics including: parallel medicinal chemistry; solid supported reagents; microwave assisted chemistry; flow synthesis, and high throughput reaction screening.
Flow Chemistry for the Synthesis of Heterocycles by Upendra K. Sharma,Erik V. Van der Eycken Pdf
This volume provides an overview of recent developments and scope in the use of flow chemistry in relevance to heterocyclic synthesis. The heterocyclic ring is the most prominent structural motif in the vast majority of natural products as well as pharmaceutical compounds since this facilitates tuneable interactions with the biological target besides conferring a degree of structural and metabolic stability. In recent times, flow chemistry has heralded a paradigm shift in organic synthesis as it offers several unique advantages over conventional methods like drastic acceleration of sluggish transformations, enhanced yields, cleaner reactions etc and is gradually gaining a lot of attention among organic chemist worldwide. Given the importance of heterocycles in natural products, medicinal chemistry and pharmaceuticals, this is a well warranted volume and complements the previous volume of Topics in Organometallic Chemistry ‘Organometallic Flow Chemistry’. This volume offers a versatile overview of the topic, besides discussing the recent progress in the flourishing area of flow chemistry in relevance to heterocyclic chemistry; it will also help researchers to better understand the chemistry behind these reactions. This in turn provides a platform for future innovations towards the designing of novel transformations under continuous flow. Thus, this volume will appeal to both the novices in this field as well as to experts in academia and industry.
The Application of Flow Chemistry to the Synthesis of Pharmaceutically Privileged Heterocycles by Blake Jamie Mark Baker Pdf
This thesis describes the development and use of flow methods in the synthesis of medicinally privileged heterocycles. As a developing technology, advances in the understanding and technological hardware involved within flow chemistry have resulted in its widespread employment throughout the chemical sector. Specifically, factors including the ease of in-line analysis and streamlining of multi-step syntheses, as well as benefits offered in safety control, heating efficiency, reagent addition control, uniformity of performance and facile upscaling, and the reduced footprint of reactors in comparison to traditional batch methods have appreciably added to the value and applicability of this technique, especially in large scale synthetic procedures. Despite this, the majority of early-stage research and discovery chemistry still relies on the use of batch reactions. As a result, and in a drive to utilise state-of-the-art technology within our laboratory in order to redefine drug discovery practices, this work presents the use of flow chemistry within two distinct, and highly relevant applications. Imidazoheterocycles are motifs of foremost importance to the medicinal chemistry community, being present in clinical candidates and probes for a number of health indications. As a result, an effective and reliable synthetic preparation for their access and isolation would be invaluable. The first chapter involves the use of a combination of commercial flow apparatus to develop a chemical methodology for the efficient, sustainable, scalable and robust synthesis of aminated imidazoheterocycles via the Groebke-Blackburn-Bienaymé multicomponent reaction. Advantages of this process include the requirement for a reaction (residence) time of only 50 minutes, the tolerance of a wide range of functionality in all starting materials, and the facile scalability in flow, as demonstrated on multi-gram scale. A smaller, bespoke microfluidic system was then applied for the second chapter, where the use of flow equipment was validated in an ongoing programme within our laboratories, to rapidly generate a small library of diaminoquinazolines as potential antimalarials, following on from work at GSK's infectious disease site in Tres Cantos, Madrid. Computational design elements were used to select small molecule targets based on frequently considered physicochemical parameters, and a tandem SNAr method was employed to produce decorated heterocyclic products in a short overall reaction time. This process represents a substantial acceleration in the synthesis of these compounds, facilitating far-reaching future work involving rapid drug design and access, and the potential for streamlining the preparative methods between small- and large-scale chemistry within early-stage discovery, especially within the pharmaceutical industry.
This ready reference not only presents the hot and emerging topic of modern flow chemistry, it is also unique in illustrating the important connection to sustainable chemistry. Focusing on more sustainable methods and applications, the text extensively covers every important field from reaction time optimization to waste minimization, and from safety improvements to microwave applications. In addition, green metrics are presented as a key aspect of the book, helping readers to evaluate the efficiency of flow technologies and their impact on the overall efficiency of a chemical process. An invaluable handbook for every chemist working in the laboratory, whether in academia or industry.
Author : Emily A. Peterson,Julie B. Manley Publisher : Royal Society of Chemistry Page : 338 pages File Size : 41,8 Mb Release : 2015-06-30 Category : Medical ISBN : 9781849739610
Green Chemistry Strategies for Drug Discovery by Emily A. Peterson,Julie B. Manley Pdf
The incorporation of Green Chemistry is a relatively new phenomenon in the drug discovery discipline, since the scale that chemists operate on in drug discovery is smaller than those of process and manufacturing chemistry. The necessary metrics are more difficult to obtain in drug discovery due to the diversity of reactions conducted. However, pharmaceutical companies are realizing that incorporation of green chemistry techniques at earlier stages of drug development can speed the development of a drug candidate. Edited by experts who have pioneered green chemistry efforts within their own institutions, this book provides a practical guide for both academic and industrial labs wanting to know where to start with introducing greener approaches for greatest return on investment. The Editors have taken a comprehensive approach to the topic covering the entire drug discovery process from molecule conception, through synthesis, formulation and toxicology with specific examples and case studies where green chemistry strategies have been implemented. Currently employed as well as emerging techniques for performing greener drug discovery chemistry are addressed as well as cutting-edge topics like biologics discovery. Moreover, important surrounding issues such as intellectual property are included. This book will serve as a practical guide for both academic and industrial chemists who work across the breadth of the drug discovery discipline. Ultimately, readers will learn how to incorporate green chemistry strategies into their everyday workflow without slowing down their science.
Flow Cytometry in Drug Discovery and Development by Virginia Litwin,Philip Marder Pdf
This book covers the unique application of flow cytometry in drug discovery and development. The first section includes two introductory chapters, one on flow cytometry and one on biomarkers, as well as a chapter on recent advances in flow cytometry. The second section focuses on the unique challenges and added benefits associated with the use of flow cytometry in the drug development process. The third section contains a single chapter presenting an in depth discussion of validation considerations and regulatory compliance issues associated with drug development.
Have you ever wished you could speed up your organic syntheses without losing control of the reaction? Flash Chemistry is a new concept which offers an integrated scheme for fast, controlled organic synthesis. It brings together the generation of highly reactive species and their reactions in Microsystems to enable highly controlled organic syntheses on a preparative scale in timescales of a few seconds or less. Flash Chemistry: Fast Organic Synthesis in microsystems is the first book to describe this exciting new technique, with chapters covering: an introduction to flash chemistry reaction dynamics: how fast is the act of chemical transformation, what is the rate of reaction, and what determines the selectivity of a reaction? examples of why flash chemistry is needed: the rapid construction of chemical libraries, rapid synthesis of radioactive PET probes, and on-demand rapid synthesis in industry the generation of highly reactive species through thermal, microwave, chemical, photochemical, and electrochemical activation microsystems: What are microsystems and how are they made? Why is size so important? What are the characteristic features of microsystems? conduction and control of extremely fast reactions using microsystems applications of flash chemistry in organic synthesis polymer synthesis based on flash chemistry industrial applications of flash chemistry Flash Chemistry: Fast Organic Synthesis in Microsystems is an essential introduction to anyone working in organic synthesis, process chemistry, chemical engineering and physical organic chemistry concerned with fundamental aspects of chemical reactions an d synthesis and the production of organic compounds.
Green Chemistry in Drug Discovery by Paul F. Richardson Pdf
This detailed book highlights several emerging areas in the implementation of green chemistry in medicinal chemistry drug discovery with a specific focus on their application to the expeditious discovery of new biologically active entities. Divided into three sections, the collection explores greener approaches to chemical transformations that are both prevalent and have been highlighted as challenging within the pharmaceutical industry, overall synthetic strategy, as well as the implementation and impact of a range of enabling technologies within medicinal chemistry. As a volume of the Methods in Pharmacology and Toxicology series, chapters provide the kind of key insight that can guide researchers toward greater success in the lab. Authoritative and practical, Green Chemistry in Drug Discovery: From Academia to Industry provides both a fundamental insight into the progress that has been made as well as some of the challenges that still exist for these techniques to be effectively implemented in the drug discovery process in a routine manner.
Efficiency in Natural Product Total Synthesis by Pei-Qiang Huang,Zhu-Jun Yao,Richard P. Hsung Pdf
Uniting the key organic topics of total synthesis and efficient synthetic methodologies, this book clearly overviews synthetic strategies and tactics applied in total synthesis, demonstrating how the total synthesis of natural products enables scientific and drug discovery. • Focuses on efficiency, a fundamental and important issue in natural products synthesis that makes natural product synthesis a powerful tool in biological and pharmaceutical science • Describes new methods like organocatalysis, multicomponent and cascade reactions, and biomimetic synthesis • Appeals to graduate students with two sections at the end of each chapter illustrating key reactions, strategies, tactics, and concepts; and good but unfinished total synthesis (synthesis of core structure) before the last section • Compiles examples of solid phase synthesis and continuing flow chemistry-based total synthesis which are very relevant and attractive to industry R&D professionals
Applications by Ferenc Darvas,Volker Hessel,György Dorman Pdf
"Flow Chemistry fills the gap in graduate education by covering chemistry and reaction principles along with current practice, including examples of relevant commercial reaction, separation, automation, and analytical equipment. The Editors of Flow Chemistry are commended for having taken the initiative to bring together experts from the field to provide a comprehensive treatment of fundamental and practical considerations underlying flow chemistry. It promises to become a useful study text and as well as reference for the graduate students and practitioners of flow chemistry." Professor Klavs Jensen Massachusetts Institute of Technology, USA Broader theoretical insight in driving a chemical reaction automatically opens the window towards new technologies particularly to flow chemistry. This emerging concept promotes the transformation of present day's organic processes into a more rapid continuous set of synthesis operations, more compatible with the envisioned sustainable world. These two volumes Fundamentals and Applications provide both the theoretical foundation as well as the practical aspects.
Catalytic Methods in Flow Chemistry by Christophe Len,Renzo Luisi Pdf
The chemical industry is essential in the daily humn life of modern society; despite the misconception about the real need for chemical production, everyone enjoys the benefit of the chemical progress. However, the chemical industry generates a large variety of products, including (i) basic chemicals, e.g., polymers, petrochemicals, and basic inorganics; (ii) specialty chemicals for crop protection, paints, inks, colorants, textiles, paper, and engineering; and (iii) consumer chemicals, including detergents, soaps, etc. For these reasons, chemists in both acdemia and industry are challenged with developing green and sustainable chemical production towrad the full-recycling of feedstocks and waste. Aiming to improve the intensification of the process, chemists have established chemical reactions based on catalysis, as well as alternative technologies, such as continuous flow. The aim of this book is to cover promising recent research and novel trends in the field of novel catalytic reactions (homogeneous, heterogeneous, and enzymatic, as well as their combinations) in continuous flow conditions. A collection of recent contribution for conversion of starting material originated from petroleum resources or biomass into highly-added value chemicals are reported.
Author : David C. Blakemore,Paul M. Doyle,Yvette M. Fobian Publisher : Royal Society of Chemistry Page : 536 pages File Size : 48,7 Mb Release : 2016 Category : Drug development ISBN : 9781782627869
Synthetic Methods in Drug Discovery by David C. Blakemore,Paul M. Doyle,Yvette M. Fobian Pdf
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.
