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Synthesis Of The C1 C9 Fragment Of Disorazole C1 And Novel Heterocyclic Analogues
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Book Synopsis Synthesis of the C(1)-C(9) Fragment of Disorazole C1 and Novel Heterocyclic Analogues by : Helen Sarah Niblock
Download or read book Synthesis of the C(1)-C(9) Fragment of Disorazole C1 and Novel Heterocyclic Analogues written by Helen Sarah Niblock and published by . This book was released on 2012 with total page 214 pages. Available in PDF, EPUB and Kindle. Book excerpt: A highly convergent strategy for the synthesis of the antitubulin polyketide disorazole C1 is proposed based around the alkyne precursor I, featuring a novel Evans-Tishchenko/ring closing alkyne metathesis approach. Due to the inherent symmetry of the molecule this retrosynthesis leads to two fragments: a [beta]- hydroxyketone II and the oxazole C(1)-(9) fragment III. A review of previous syntheses of disorazole C1 and established structure activity relationships (SARs) highlights a gap in current knowledge relating to the role of the oxazole in tubulin binding. Therefore, the focus of this research has been towards developing new routes for the synthesis of the C(1)-C(9) fragment that can be adapted to the synthesis of heterocyclic analogues to further establish the SAR of disorazole C1. Chapter 2 focuses on a disconnection at the C(5)-C(6) bond and a novel synthesis of the racemic C(1)-C(9) fragment has been achieved via a lithiation of methyl 2- methyl-1,3-oxazole-4-carboxylate and coupling to aldehyde V. First generation asymmetric routes to the C(1)-C(9) fragment centred on i. a biomimetic amino acid condensation route via an oxazoline intermediate based on the precedent of Meyers et al. and ii. a C(4)-C(5) disconnection approach based around the epoxide VII; are discussed in chapter 3. A second generation C(4)-C(5) disconnection centred on the novel tosylate VIII is discussed in chapter 4. Attempts to synthesise the parent C(1)- C(9) oxazole fragment using the tosylate VIII via i. a palladium catalysed C-H activation of ethyl 4-oxazole carboxylate and ii. lithiation of oxazole are reported. Coupling of fragment VIII (X = OTs) with ethyl 1H-pyrazole-4-carboxylate and a CuAAC coupling of the azide derived from tosylate VIII with methyl propiolate has allowed the successful completion of the synthesis of pyrazole and triazole analogues of this fragment.
Book Synopsis Studies Towards the Total Synthesis of Disorazole C1 and Its Analogues by : Kevin John Ralston
Download or read book Studies Towards the Total Synthesis of Disorazole C1 and Its Analogues written by Kevin John Ralston and published by . This book was released on 2014 with total page pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis (-)-disorazole C1 and New Analogs by : Luca Lizzadro
Download or read book (-)-disorazole C1 and New Analogs written by Luca Lizzadro and published by . This book was released on 2022 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Applied Cross-Coupling Reactions by : Yasushi Nishihara
Download or read book Applied Cross-Coupling Reactions written by Yasushi Nishihara and published by Springer Science & Business Media. This book was released on 2012-12-14 with total page 247 pages. Available in PDF, EPUB and Kindle. Book excerpt: “Applied Cross-Coupling Reactions” provides students and teachers of advanced organic chemistry with an overview of the history, mechanisms and applications of cross-coupling reactions. Since the discovery of the transition-metal-catalyzed cross-coupling reactions in 1972, numerous synthetic uses and industrial applications have been developed. The mechanistic studies of the cross-coupling reactions have disclosed that three fundamental reactions: oxidative addition, transmetalation, and reductive elimination, are involved in a catalytic cycle. Cross-coupling reactions have allowed us to produce a variety of compounds for industrial purposes, such as natural products, pharmaceuticals, liquid crystals and conjugate polymers for use in electronic devices. Indeed, the Nobel Prize for Chemistry in 2010 was awarded for work on cross-coupling reactions. In this book, the recent trends in cross-coupling reactions are also introduced from the point of view of synthesis design and catalytic activities of transition-metal catalysts.
Book Synopsis Organophosphorus Chemistry by : David W Allen
Download or read book Organophosphorus Chemistry written by David W Allen and published by Royal Society of Chemistry. This book was released on 2020-04-15 with total page 410 pages. Available in PDF, EPUB and Kindle. Book excerpt: This annual review of the literature presents a comprehensive and critical survey of the vast field of study involving organophosphorus compounds, from phosphines and related P-C bonded compounds to phosphorus acids, phosphine chalcogenides and nucleotides. The Editors have added to the content with a timely chapter on the recent developments in green synthetic approaches in organophosphorus chemistry to reflect current interests in the area. With an emphasis on interdisciplinary content, this book is aimed at the worldwide organic chemistry and engineering research communities.
Book Synopsis Total Synthesis of Natural Products by : Jie Jack Li
Download or read book Total Synthesis of Natural Products written by Jie Jack Li and published by Springer Science & Business Media. This book was released on 2013-03-14 with total page 292 pages. Available in PDF, EPUB and Kindle. Book excerpt: 'Total Synthesis of Natural Products' is written and edited by some of today's leaders in organic chemistry. Eleven chapters cover a range of natural products, from steroids to alkaloids. Each chapter contains an introduction to the natural product in question, descriptions of its biological and pharmacological properties and outlines of total synthesis procedures already carried out. Particular emphasis is placed on novel methodologies developed by the respective authors and their research groups. This text is ideal for graduate and advanced undergraduate students, as well as organic chemists in academia and industry.
Book Synopsis Modern Enolate Chemistry by : Manfred Braun
Download or read book Modern Enolate Chemistry written by Manfred Braun and published by John Wiley & Sons. This book was released on 2016-02-23 with total page 454 pages. Available in PDF, EPUB and Kindle. Book excerpt: Authored by one of the world?s leading synthetic chemists in the field, this reference presents modern enolate chemistry with an emphasis on metal O-enolates in asymmetric synthesis. While great care is taken to cover novel, successful concepts, such classical methods as the famous Evans enolates are equally highlighted. Throughout the book representative reaction procedures are presented, thus helping readers to find the best solution for their own synthetic problem. Of high interest to synthetic chemists in academia, as well as the pharmaceuticals, agrochemicals and fine chemicals industries.
Book Synopsis Marine Natural Products by : Hiromasa Kiyota
Download or read book Marine Natural Products written by Hiromasa Kiyota and published by Springer. This book was released on 2010-11-11 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Anticancer Agents from Natural Products by : Gordon M. Cragg
Download or read book Anticancer Agents from Natural Products written by Gordon M. Cragg and published by CRC Press. This book was released on 2005-06-13 with total page 610 pages. Available in PDF, EPUB and Kindle. Book excerpt: Plants, marine organisms, and microorganisms have evolved complex chemical defense and signaling systems that are designed to protect them from predators and provide other biological benefits. These organisms thus produce substances containing novel chemotypes that may have beneficial effects for humans. As collection methods improve and new screen
Book Synopsis Handbook of Metathesis, 3 Volume Set by : Robert H. Grubbs
Download or read book Handbook of Metathesis, 3 Volume Set written by Robert H. Grubbs and published by John Wiley & Sons. This book was released on 2015-05-26 with total page 1639 pages. Available in PDF, EPUB and Kindle. Book excerpt: Covering the complete breadth of the olefin metathesis reaction. The second edition of the ultimate reference in this field is completely updated and features more than 80% new content, with the focus on new developments in the field, especially in industrial applications. No other book covers the topic in such a comprehensive manner and in such high quality, and this new edition retains the three-volume format: Catalyst Development, Applications in Organic Synthesis and Polymer Synthesis. Edited by a Nobel laureate in the field, and with a list of contributors that reads like a "Who's-Who" of metathesis, this is an indispensable one-stop reference for organic, polymer and industrial chemists, as well as chemists working with organometallics. Individual volumes also available separately to purchase Volume 1: Catalyst Development - http://www.wiley.com/WileyCDA/WileyTitle/productCd-3527339485.html Volume 2: Applications in Organic Synthesis - http://www.wiley.com/WileyCDA/WileyTitle/productCd-3527339493.html Volume 3: Polymer Synthesis - http://www.wiley.com/WileyCDA/WileyTitle/productCd-3527339507.html
Book Synopsis Molecules and Medicine by : E. J. Corey
Download or read book Molecules and Medicine written by E. J. Corey and published by John Wiley & Sons. This book was released on 2012-02-28 with total page 272 pages. Available in PDF, EPUB and Kindle. Book excerpt: Molecules and Medicine provides, for the first time ever, a completely integrated look at chemistry, biology, drug discovery, and medicine. It delves into the discovery, application, and mode of action of more than one hundred of the most significant molecules in use in modern medicine. Opening sections of the book provide a unique, clear, and concise introduction, which enables readers to understand chemical formulas.
Download or read book Macrocycles written by E. Weber and published by Springer. This book was released on 1992 with total page 298 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Book Synopsis Modern Alkaloids by : Ernesto Fattorusso
Download or read book Modern Alkaloids written by Ernesto Fattorusso and published by John Wiley & Sons. This book was released on 2008-01-08 with total page 689 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book presents all important aspects of modern alkaloid chemistry, making it the only work of its kind to offer up-to-date and comprehensive coverage. While the first part concentrates on the structure and biology of bioactive alkaloids, the second one analyzes new trends in alkaloid isolation and structure elucidation, as well as in alkaloid synthesis and biosynthesis. A must for biochemists, organic, natural products, and medicinal chemists, as well as pharmacologists, pharmaceutists, and those working in the pharmaceutical industry.
Download or read book Olefin Metathesis written by Karol Grela and published by . This book was released on 2014 with total page 608 pages. Available in PDF, EPUB and Kindle. Book excerpt: This is a complete examination of the theory and methods of modern olefin metathesis, one of the most widely used chemical reactions in research and industry. Provides basic information for non-specialists, while also explaining the latest trends and advancements in the field to experts Discusses the various types of metathesis reactions, including CM, RCM, enyne metathesis, ROMP, and tandem processes, as well as their common applications Outlines the tools of the trade--from the important classes of active metal complexes to optimal reaction conditions--and suggests practical solutions for common reaction problems Includes tables with structures of commercial catalysts, and recommendations for commercial catalyst suppliers
Book Synopsis Recent Progress in the Chemical Synthesis of Antibiotics by : Gabor Lukacs
Download or read book Recent Progress in the Chemical Synthesis of Antibiotics written by Gabor Lukacs and published by Springer Science & Business Media. This book was released on 2012-12-06 with total page 808 pages. Available in PDF, EPUB and Kindle. Book excerpt: The use of antibiotics in the treatment by antibacterial and antifungal chemo therapy, has become standard practice since the end of World War Two and has had an enormous impact on healthcare throughout the world. Compounds belonging to this class have also reached an important place in the medical treatment of human cancer. Although, the discovery of most of these agents came from more or less sophisticated screening programs of soil microrganisms, many of the important antibiotics used today in clinical practice are derived from the original biosynthetic products by the application of often novel and generally elaborated chemical synthetic methodologies. In fact the antibiotics have represented (and still represent) for a generation of organic chemists an endless source of molecular structures whose varied assemblage of carbon atom backbones and chemical functions was beyond any possibility of imagination. Perhaps a similar repertoire of chemotypes was formerly offered by the natural products, namely the alkaloids, the terpenes, the vitamins and hormones as well as the pigments of the animal and plant kingdoms, albeit the chemical arrange ments of the antibiotic molecules appeared much more surprising and diverse to the admiring eyes of cultivated organic chemists. The idea of this book, certainly a landmark in the field, came during the Symposium of EUCHEM on Chemical Synthesis of Antibiotics, that was held at Aussois in Savoy, France (May 2-6, 1988), the initiative being taken by Gabor Lukacs to whom Masaji Ohno readily associated as a co-editor.
Book Synopsis Molecules That Changed the World by : K. C. Nicolaou
Download or read book Molecules That Changed the World written by K. C. Nicolaou and published by Wiley-VCH. This book was released on 2008-03-17 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: K.C. Nicolaou - Winner of the Nemitsas Prize 2014 in Chemistry Here, the best-selling author and renowned researcher, K. C. Nicolaou, presents around 40 natural products that all have an enormous impact on our everyday life. Printed in full color throughout with a host of pictures, this book is written in the author's very enjoyable and distinct style, such that each chapter is full of interesting and entertaining information on the facts, stories and people behind the scenes. Molecules covered span the healthy and useful, as well as the much-needed and extremely toxic, including Aspirin, urea, camphor, morphine, strychnine, penicillin, vitamin B12, Taxol, Brevetoxin and quinine. A veritable pleasure to read.
Book Synopsis Lead Generation Approaches in Drug Discovery by : Zoran Rankovic
Download or read book Lead Generation Approaches in Drug Discovery written by Zoran Rankovic and published by John Wiley & Sons. This book was released on 2010-04-07 with total page 310 pages. Available in PDF, EPUB and Kindle. Book excerpt: An integrated overview of modern approaches to lead discovery Lead generation is increasingly seen as a distinct and success-determining phase of the drug discovery process. Over recent years, there have been major advances in the understanding of what constitutes a good lead compound and how to improve the chances of finding such a compound. Written by leading scientists and established opinion leaders from industry and academia, this book provides an authoritative overview of the field, as well as the theory, practice, and scope, of the principal Lead Generation Approaches in Drug Discovery, including: The evolution of the lead discovery process, key concepts, current challenges, and future directions Strategies and technologies driving the high-throughput screening (HTS) approach to lead discovery, including the shifting paradigms in the design of compound collections and best practice in the hit confirmation process Knowledge-based in silico or "virtual" screening Theory and practice of the fragment-based approach to lead discovery The opportunities and challenges presented by multi-target drug discovery (MTDD) De novo design of lead compounds and new approaches to estimating the synthetic accessibility of de novo–designed molecules The impact of natural products on drug discovery, and potential of natural product–like compounds for exploring regions of biologically relevant chemical space Using early screening of hits and leads for metabolic, pharmacokinetic, and toxicological liabilities to reduce attrition during the later phases of drug discovery The utility of parallel synthesis and purification in lead discovery With each topic supported by numerous case studies, this is indispensable reading for researchers in industry and academia who wish to keep up to date with the latest strategies and approaches in drug discovery.
