Author: Alexandru GheorghePublisher:
ISBN:
Category :
Languages : en
Pages :
Book Description
Development of New Methods for the Synthesis of Pharmacologically Active Compounds
Author: Alexandru GheorgheFundamentals of Early Clinical Drug Development
Author: Ahmed F. Abdel-MagidPublisher: John Wiley & Sons
ISBN: 0470043393
Category : Science
Languages : en
Pages : 341
Book Description
An informative look at the intricacies of today's drug development process Once a discovery organization has identified a potential new drug candidate, it is the daunting task of synthetic organic chemists to identify the chemical process suitable for preparation of this compound in a highly regulated environment. Only through a multi-layered chemical process that takes into account such factors as safety, environmental considerations, freedom to operate and cost-effectiveness can researchers begin to refine the drug in terms of quality and yield. This book covers both recent advances in the design and synthesis of new drugs, as well as the myriad other issues facing a new drug candidate as it moves through the development process. Utilizing recent case studies, the authors provide valuable insights into the complexities of the process, from designing new synthetic methodologies and applying new automated techniques for finding optimal reaction conditions to selecting the final drug form and formulation. Both novice and active researchers will appreciate the inclusion of chapters on such diverse topics as: * Cross-coupling methods * Asymmetric synthesis * Automation * Chemical Engineering * Application of radioisotopes * Final form selection * Formulations * Intellectual property A wealth of real-world examples and contributions from leading process scientists, engineers, and related professionals make this book a valuable addition to the scientific literature.
Flow Chemistry in Drug Discovery
Author: Jesus AlcazarPublisher: Springer Nature
ISBN: 3030855929
Category : Science
Languages : en
Pages : 501
Book Description
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.
Strategies for Organic Drug Synthesis and Design
Author: Daniel LednicerPublisher: John Wiley & Sons
ISBN: 9780470399590
Category : Science
Languages : en
Pages : 700
Book Description
This book examines and evaluates the strategies utilized to design and synthesize pharmaceutically active agents. Significant updates over the last 10 years since the publication of the 1st edition include synthesis of enantiomerically pure isomers, novel chemical methodologies, and new pharmaceutical agents targeted at novel biological endpoints. Written by an experienced successful author, this book meets the needs of a growing community of researchers in pharmaceutical R &D, as well as medical professionals, by providing a useful guide for designing and synthesizing pharmaceutical agents. Additionally, it is a useful text for medicinal chemistry students.
Drug-like Properties: Concepts, Structure Design and Methods
Author: Li DiPublisher: Elsevier
ISBN: 0080557619
Category : Science
Languages : en
Pages : 549
Book Description
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. Serves as an essential working handbook aimed at scientists and students in medicinal chemistry Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies Discusses improvements in pharmacokinetics from a practical chemist's standpoint
Synthesis of Best-Seller Drugs
Author: Ruben VardanyanPublisher: Academic Press
ISBN: 0124115241
Category : Medical
Languages : en
Pages : 870
Book Description
Synthesis of Best-Seller Drugs is a key reference guide for all those involved with the design, development, and use of the best-selling drugs. Designed for ease of use, this book provides detailed information on the most popular drugs, using a practical layout arranged according to drug type. Each chapter reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and synthesis. Of high interest to all those who work in the captivating areas of biologically active compounds and medicinal drug synthesis, in particular medicinal chemists, biochemists, and pharmacologists, the book aims to support current research efforts, while also encouraging future developments in this important field. Describes methods of synthesis, bioactivity and related drugs in key therapeutic areas Reviews the main drugs in each of nearly 40 key therapeutic areas, also examining their classification, novel structural features, models of action, and more Presents a practical layout designed for use as a quick reference tool by those working in drug design, development and implementation
The Organic Chemistry of Drug Design and Drug Action
Author: Richard B. SilvermanPublisher: Elsevier
ISBN: 0080513379
Category : Science
Languages : en
Pages : 650
Book Description
Standard medicinal chemistry courses and texts are organized by classes of drugs with an emphasis on descriptions of their biological and pharmacological effects. This book represents a new approach based on physical organic chemical principles and reaction mechanisms that allow the reader to extrapolate to many related classes of drug molecules. The Second Edition reflects the significant changes in the drug industry over the past decade, and includes chapter problems and other elements that make the book more useful for course instruction. New edition includes new chapter problems and exercises to help students learn, plus extensive references and illustrations Clearly presents an organic chemist's perspective of how drugs are designed and function, incorporating the extensive changes in the drug industry over the past ten years Well-respected author has published over 200 articles, earned 21 patents, and invented a drug that is under consideration for commercialization
Technological Innovation
Author: Annetine C. GelijnsPublisher: National Academies
ISBN:
Category : Clinical medicine
Languages : en
Pages : 78
Book Description
New Synthetic Methodologies Directed Toward Pharmacologically Active Compounds as Well as Silole Based Chromophores for Analytical and Optoelectronic Applications
Author: Mahmoud M. Abd Rabo MoustafaPublisher:
ISBN:
Category :
Languages : en
Pages :
Book Description
The development of new and efficient synthetic methodologies to prepare heterocyclic compounds has received great attention over the years due to their importance in the pharmaceuticals and fine chemicals industries. Described herein are several novel syntheses of a variety of heterocycles including siloles, azaindoles, piperideines, piperidines and tetrahydropyrans. A one-pot, two-step methodology involving Tamao's reductive cyclization followed by Negishi cross coupling was utilized to synthesize several new series of silole-based chromophores. The property studies revealed new electropolymerized poly(thienyl-silole)s with enhanced photoefficiency for all-polymer solar cells. In addition, a new procedure is developed for the synthesis of the first dissymmetric silole tethered to amine functionality. The synthesized compounds hold great promise in the arena of biosensors and solar cell applications. Furthermore, a novel and practical two step sequence for the preparation of C2 substituted 5-azaindoles has been reported. The synthetic sequence features a [3+2] dipolar cycloaddition between nitriles and a 3,4-cyclopropanopiperidine followed by SeO2 oxidation. Finally, the annulation reaction between 2-alkoxy-1,1-cyclobutane diesters and imines or aldehydes gave access to highly functionalized piperidines and tetrahydropyrans, respectively. Both the synthesis of those donor-acceptor cyclobutanes and their subsequent annulations are catalyzed by catalytic Yb(OTf)3. Although known for more than two decades, this is the first use of 2-alkoxy-1,1-cyclobutane diesters in dipolar cycloadditions. The new reactions are done under mild conditions providing the target compounds in high yields and excellent selectivity. The divergent nature and cost effectiveness of these methods make them very suitable for combinatorial applications in the pharmaceutical industry. The new reactions are done under mild conditions providing the target compounds in high yields and excellent selectivity. The divergent nature and cost effectiveness of these methods make them very suitable for combinatorial applications in the pharmaceutical industry.
Flow Chemistry in Drug Discovery
Author: Jesus AlcazarPublisher:
ISBN: 9783030855932
Category :
Languages : en
Pages : 0
Book Description
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.