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Retrosynthesis in the Manufacture of Generic Drugs

Retrosynthesis in the Manufacture of Generic Drugs
Author: Pedro Paulo Santos
Publisher: John Wiley & Sons
Total Pages: 436
Release: 2020-11-09
Genre: Science
ISBN: 1119155533

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Offers a compendium of information on retrosynthesis and process chemistry, featuring innovative "reaction maps" showing synthetic routes of some widely used drugs This book illustrates how the retrosynthetic tool is applied in the Pharmaceutical Industry. It considers and evaluates the many viable synthetic routes that can be used by practicing industrialists, guiding readers through the various steps that lead to the "best" processes and the limits encountered if these are put into practice on an industrial scale of seven key Active Pharmaceutical Ingredient (API). It presents an evaluation of the potential each process has for implementation, before merging the two points of view—of retrosynthesis and process chemistry—in order to show how retrosynthetic analysis assists in selecting the most efficient route for an industrial synthesis of a particular compound whilst giving insight into the industrial process. The book also uses some key concepts used by process chemists to improve efficiency to indicate the best route to select. Each chapter in Retrosynthesis in the Manufacture of Generic Drugs Selected Case Studies is dedicated to one drug, with each containing information on: worldwide sales and patent status of the Active Pharmaceutical Ingredient (API); structure analysis and general retrosynthetic strategy of the API; first reported synthesis; critical analysis of the processes which have been developed and comparison of the synthetic routes; lessons learned; reaction conditions for Schemes A to X; chemical "highlights" on key reactions used during the synthesis; and references. Drugs covered include: Gabapentin, Clopidogrel, Citalopram and Escitalopram, Sitagliptin, Ezetimibe, Montelukast, and Oseltamivir. Show how the retrosynthetic tool is used by the Pharmaceutical Industry Fills a gap for a book where retrosynthetic analysis is systematically applied to active pharmaceutical ingredients (APIs) Features analyses and methodologies that aid readers in uncovering practical synthetic routes to other drug substances, whether they be NCEs (New Chemical Entities) or generic APIs (Active Pharmaceutical Ingredients) Presents information from both the patent and academic literature for those who wish to use as a basis for further study and thought Features the use of "reaction maps" which display several synthetic processes in the same scheme, and which allow easy comparisons of different routes that give the same molecule or intermediate. A selection of these maps are available to download from: https://www.wiley.com/go/santos/retrosynthesis Retrosynthesis in the Manufacture of Generic Drugs Selected Case Studies is an ideal book for researchers and advanced students in organic synthetic chemistry and process chemistry. It will also be of great benefit to practitioners in the pharmaceutical industry, particularly new starters, and those new to process chemistry.


Synthesis of Essential Drugs

Synthesis of Essential Drugs
Author: Ruben Vardanyan
Publisher: Elsevier
Total Pages: 635
Release: 2006-03-10
Genre: Medical
ISBN: 008046212X

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Synthesis of Essential Drugs describes methods of synthesis, activity and implementation of diversity of all drug types and classes. With over 2300 references, mainly patent, for the methods of synthesis for over 700 drugs, along with the most widespread synonyms for these drugs, this book fills the gap that exists in the literature of drug synthesis. It provides the kind of information that will be of interest to those who work, or plan to begin work, in the areas of biologically active compounds and the synthesis of medicinal drugs. This book presents the synthesis of various groups of drugs in an order similar to that traditionally presented in a pharmacology curriculum. This was done with a very specific goal in mind – to harmonize the chemical aspects with the pharmacology curriculum in a manner useful to chemists. Practically every chapter begins with an accepted brief definition and description of a particular group of drugs, proposes their classification, and briefly explains the present model of their action. This is followed by a detailed discussion of methods for their synthesis. Of the thousands of drugs existing on the pharmaceutical market, the book mainly covers generic drugs that are included in the WHO’s Essential List of Drugs. For practically all of the 700+ drugs described in the book, references (around 2350) to the methods of their synthesis are given along with the most widespread synonyms. Synthesis of Essential Drugs is an excellent handbook for chemists, biochemists, medicinal chemists, pharmacists, pharmacologists, scientists, professionals, students, university libraries, researchers, medical doctors and students, and professionals working in medicinal chemistry. * Provides a brief description of methods of synthesis, activity and implementation of all drug types* Includes synonyms* Includes over 2300 references


Fundamentals of Medicinal Chemistry

Fundamentals of Medicinal Chemistry
Author: Gareth Thomas
Publisher: John Wiley & Sons
Total Pages: 302
Release: 2004-04-20
Genre: Science
ISBN: 0470871695

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Provides a concise introduction to the chemistry of therapeutically active compounds, written in a readable and accessible style. The title begins by reviewing the structures and nomenclature of the more common classes of naturally occurring compounds found in biological organisms. An overview of medicinal chemistry is followed by chapters covering the discovery and design of drugs, pharmacokinetics and drug metabolism, The book concludes with a chapter on organic synthesis, followed by a brief look at drug development from the research stage through to marketing the final product. The text assumes little in the way of prior biological knowledge. relevant biology is included through biological topics, examples and the Appendices. Incorporates summary sections, examples, applications and problems Each chapter contains an additional summary section and solutions to the questions are provided at the end of the text Invaluable for undergraduates studying within the chemical, pharmaceutical and life sciences.


Drug Synthesis Book Set

Drug Synthesis Book Set
Author: Jie Jack Li
Publisher: John Wiley & Sons
Total Pages: 0
Release: 2015-11-23
Genre: Science
ISBN: 9781119185659

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This set presents the authoritative and acclaimed Drug Synthesis books edited by Jie Jack Li and Douglas Johnson: Contemporary Drug Synthesis, The Art of Drug Synthesis, Modern Drug Synthesis, and Innovative Drug Synthesis. This book set will be enormously useful to pharmaceutical industry labs, research scientists in lead optimization and process development, and graduate students and courses in organic chemistry, synthetic organic chemistry, heterocyclic chemistry, medicinal chemistry, and drug synthesis courses.


Modern Drug Synthesis

Modern Drug Synthesis
Author: Jie Jack Li
Publisher: John Wiley & Sons
Total Pages: 371
Release: 2013-03-27
Genre: Science
ISBN: 1118701240

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Following Contemporary Drug Synthesis and The Art of Drug Synthesis (Wiley, 2004 and 2007), two well-received works, is this new book that demystifies the process of modern drug discovery for practitioners and students. An enhanced introduction covers areas such as background, pharmacology, SAR, PK/PD, efficacy, and safety. Focusing on the advantages of process synthesis versus the discovery synthetic route, Modern Drug Synthesis features authoritative coverage by distinguished editors and authors (some chapter authors are the actual inventor of the drug) of twenty different drug molecules.


Chemistry and Analysis of Radionuclides

Chemistry and Analysis of Radionuclides
Author: Jukka Lehto
Publisher: John Wiley & Sons
Total Pages: 405
Release: 2011-01-19
Genre: Science
ISBN: 3527633022

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Written by chemists for chemists, this is a comprehensive guide to the important radionuclides as well as techniques for their separation and analysis. It introduces readers to the important laboratory techniques and methodologies in the field, providing practical instructions on how to handle nuclear waste and radioactivity in the environment.


Industrial Pharmaceutical Biotechnology

Industrial Pharmaceutical Biotechnology
Author: Heinrich Klefenz
Publisher: Wiley-VCH
Total Pages: 328
Release: 2002-04-22
Genre: Medical
ISBN:

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This volume focuses on pharmaceutical biotechnology as a key area of life sciences. The complete range of concepts, processes and technologies of biotechnology is applied in modern industrial pharmaceutical research, development and production. The results of genome sequencing and studies of biological-genetic function are combined with chemical, micro-electronic and microsystem technology to produce medical devices and diagnostic biochips. A multitude of biologically active molecules is expanded by additional novel structures created with newly arranged gene clusters and bio-catalytic chemical processes. New organisational structures in the co-operation of institutes, companies and networks enable faster knowledge and product development and immediate application of the results of research and process development. This book is the ideal source of information for scientists and engineers in research and development, for decision-makers in biotech, pharma and chemical corporations, as well as for research institutes, but also for founders of biotech companies and people working for venture capital corporations.


Organic Chemistry from Retrosynthesis to Asymmetric Synthesis

Organic Chemistry from Retrosynthesis to Asymmetric Synthesis
Author: Vitomir Šunjić
Publisher: Springer
Total Pages: 221
Release: 2016-04-30
Genre: Science
ISBN: 3319299263

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This book connects a retrosynthetic or disconnection approach with synthetic methods in the preparation of target molecules from simple, achiral ones to complex, chiral structures in the optically pure form. Retrosynthetic considerations and asymmetric syntheses are presented as closely related topics, often in the same chapter, underlining the importance of retrosynthetic consideration of target molecules neglecting stereochemistry and equipping readers to overcome the difficulties they may encounter in the planning and experimental implementation of asymmetric syntheses. This approach prepares students in advanced organic chemistry courses, and in particular young scientists working at academic and industrial laboratories, for independently solving synthetic problems and creating proposals for the synthesis of complex structures.


De novo Molecular Design

De novo Molecular Design
Author: Gisbert Schneider
Publisher: Wiley-VCH
Total Pages: 0
Release: 2013-12-23
Genre: Medical
ISBN: 9783527334612

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Systematically examining current methods and strategies, this ready reference covers a wide range of molecular structures, from organic-chemical drugs to peptides, Proteins and nucleic acids, in line with emerging new drug classes derived from biomacromolecules. A leader in the field and one of the pioneers of this young discipline has assembled here the most prominent experts from across the world to provide first-hand knowledge. While most of their methods and examples come from the area of pharmaceutical discovery and development, the approaches are equally applicable for chemical probes and diagnostics, pesticides, and any other molecule designed to interact with a biological system. Numerous images and screenshots illustrate the many examples and method descriptions. With its broad and balanced coverage, this will be the firststop resource not only for medicinal chemists, biochemists and biotechnologists, but equally for bioinformaticians and molecular designers for many years to come. From the content: * Reaction-driven de novo design * Adaptive methods in molecular design * Design of ligands against multitarget profiles * Free energy methods in ligand design * Fragment-based de novo design * Automated design of focused and target family-oriented compound libraries * Molecular de novo design by nature-inspired computing * 3D QSAR approaches to de novo drug design * Bioisosteres in de novo design * De novo design of peptides, proteins and nucleic acid structures, including RNA aptamers and many more.


Artificial Intelligence in Drug Discovery

Artificial Intelligence in Drug Discovery
Author: Nathan Brown
Publisher: Royal Society of Chemistry
Total Pages: 425
Release: 2020-11-04
Genre: Computers
ISBN: 1839160543

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Following significant advances in deep learning and related areas interest in artificial intelligence (AI) has rapidly grown. In particular, the application of AI in drug discovery provides an opportunity to tackle challenges that previously have been difficult to solve, such as predicting properties, designing molecules and optimising synthetic routes. Artificial Intelligence in Drug Discovery aims to introduce the reader to AI and machine learning tools and techniques, and to outline specific challenges including designing new molecular structures, synthesis planning and simulation. Providing a wealth of information from leading experts in the field this book is ideal for students, postgraduates and established researchers in both industry and academia.