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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 for Pharmaceuticals by Rodrigo Octavio Mendonca Alves de Souza Pdf
Flow chemistry offers several advantages for a change to more sustainability and flexibility in the production of pharmaceuticals. This book explains the basic concepts of flow chemistry and describes various examples for continuous synthesis and crystallization of active pharmaceutical ingredients. Recently developed techniques but also protocols already applied in industry offer a useful source for researchers in academia and professionals.
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 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.
Author : Santiago V Luis,Eduardo Garcia-Verdugo Publisher : Royal Society of Chemistry Page : 560 pages File Size : 47,5 Mb Release : 2019-10-18 Category : Science ISBN : 9781788014984
Flow Chemistry by Santiago V Luis,Eduardo Garcia-Verdugo Pdf
In flow chemistry reactions are performed in a reactor with the reactants pumped through it. It has the benefit of being easily scaled up and it is straightforward to integrate synthesis, workup and analysis into one system. This volume provides an update on recent advances in the field of flow chemistry, with special emphasis on new, integrated approaches for green and efficient chemistry. This book is a valuable resource for researchers in green chemistry, chemical engineers and Industrial chemists working in the pharmaceutical and fine chemicals industries.
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.
Science of Synthesis: Flow Chemistry in Organic Synthesis by T.F. Jamison,G. Koch Pdf
The aim of this work is to convey the practice, power, and potential of flow chemistry to a larger audience. An emerging and strengthening trend is that flow chemistry is much more than the adaption of batch processes to flow systems. Rather, flow chemistry offers a new paradigm in the way we think about chemical synthesis. This volume demonstrates the enabling power of continuous flow to access new reaction types and different chemistry space and, to this end, it has been compiled by a team of pioneers and leaders, who present both the practical and conceptual aspects of this rapidly growing field. Included are the principles of reactor design, automation, and separations/purifications in flow systems, applications in photochemistry, electrochemistry, gaseous systems, immobilized reagents and catalysts, and multistep processes. The synthesis of peptides, carbohydrates, and pharmaceuticals is covered and several chapters give insight into the use of flow in an industrial context.
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.
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.
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 : Elizabeth Farrant Publisher : Royal Society of Chemistry Page : 176 pages File Size : 42,7 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.
Middle Molecular Strategy by Koichi Fukase,Takayuki Doi Pdf
This book highlights recently discovered aspects of “middle-size molecules,” focusing on (1) their unique bio-functions on the basis of derivatives and conjugates of natural products, saccharides, peptides, and nucleotides; (2) the synthesis of structurally complex natural products; (3) special synthetic methods for π-conjugated functional molecules; and (4) novel synthetic methods using flow chemistry. Given its scope, the book is of interest to industrial researchers and graduate students in the fields of organic chemistry, medicinal chemistry, and materials science.
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.
Flow Chemistry – Applications by Ferenc Darvas,György Dormán,Volker Hessel,Steven V. Ley Pdf
The fully up-dated edition of the two-volume work covers both the theoretical foundation as well as the practical aspects. A strong insight in driving a chemical reaction is crucial for a deeper understanding of new potential technologies. New procedures for warranty of safety and green principles are discussed. Vol. 1: Fundamentals.
Powder Flow by Ali Hassanpour,Colin Hare,Massih Pasha Pdf
Powder flow has attracted increased attention in recent years as novel formulated and functional products are being developed in powder forms, particularly in pharmaceutical and high value additive manufacturing industries. This book meets a need for a truly integrated modern treatment of dry powder flow, covering theory, robust characterisation techniques, modelling tools and applications. Written by leaders in the field, the book opens by introducing the wide range of powder processing problems faced by industry, the complexities of powders and the myriad of ways their flow behaviour can be characterised. The authors then move on, with contributions from experts, to describe fundamental properties that can be measured, defining the states of stress and shear rate and the considerations that need to be taken account. By providing a comprehensive treatment of all available characterisation techniques, as well as various modelling tools, the reader obtains a clear, practical overview. Case studies and applications connect theory to practical examples across a broad range of industries. This book stands out by not only providing the reader with guidance on what to measure but also how to interpret results, ensuring this is an invaluable text for anyone working on powder flow in the chemical, pharmaceutical and manufacturing industries, as well as students and researchers across chemical and process engineering disciplines.
