New Linkers and Strategies for Solid Phase Organic Synthesis and Their Application to Natural Products Synthesis and Libraries Thereof

New Linkers and Strategies for Solid Phase Organic Synthesis and Their Application to Natural Products Synthesis and Libraries Thereof PDF Author: Nicolas Winssinger
Publisher:
ISBN: 9780599813236
Category : Alkaloids
Languages : en
Pages : 852

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Book Description
The complexity of natural products and the inherent challenges imposed by target synthesis were used as a platform to develop new strategies and linkers for solid phase organic synthesis. This research led to the development of two cyclorelease reaction involving an olefin metathesis and a Stille reaction. Our interest in linkers also led to the development of three new linkers; a simplified photolabile linker, a very versatile selenium linker and a new safety-catch linker. The utility of these developments were illustrated by the solid phase synthesis of heptasaccharide phytoalexin elicitor (HPE), epothilone A, zearalenone, sarcodictyins and vancomycin (Figure 1). Libraries of the promising anticancer agents epothilone and sarcodictyins provided valuable information towards the structure-activity relationship of these molecules as well as several compounds with improved biological activity.

New Linkers and Strategies for Solid Phase Organic Synthesis and Their Application to Natural Products Synthesis and Libraries Thereof

New Linkers and Strategies for Solid Phase Organic Synthesis and Their Application to Natural Products Synthesis and Libraries Thereof PDF Author: Nicolas Winssinger
Publisher:
ISBN: 9780599813236
Category : Alkaloids
Languages : en
Pages : 852

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Book Description
The complexity of natural products and the inherent challenges imposed by target synthesis were used as a platform to develop new strategies and linkers for solid phase organic synthesis. This research led to the development of two cyclorelease reaction involving an olefin metathesis and a Stille reaction. Our interest in linkers also led to the development of three new linkers; a simplified photolabile linker, a very versatile selenium linker and a new safety-catch linker. The utility of these developments were illustrated by the solid phase synthesis of heptasaccharide phytoalexin elicitor (HPE), epothilone A, zearalenone, sarcodictyins and vancomycin (Figure 1). Libraries of the promising anticancer agents epothilone and sarcodictyins provided valuable information towards the structure-activity relationship of these molecules as well as several compounds with improved biological activity.

Stereoselective Synthesis of Drugs and Natural Products

Stereoselective Synthesis of Drugs and Natural Products PDF Author: Vasyl Andrushko
Publisher: John Wiley & Sons
ISBN: 1118628330
Category : Science
Languages : en
Pages : 1836

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Book Description
Brings together the best tested and proven stereoselective synthetic methods Both the chemical and pharmaceutical industries are increasingly dependent on stereoselective synthetic methods and strategies for the generation of new chiral drugs and natural products that offer specific 3-D structures. With the publication of Stereoselective Synthesis of Drugs and Natural Products, researchers can turn to this comprehensive two-volume work to guide them through all the core methods for the synthesis of chiral drugs and natural products. Stereoselective Synthesis of Drugs and Natural Products features contributions from an international team of synthetic chemists and pharmaceutical and natural product researchers. These authors have reviewed the tremendous body of literature in the field in order to compile a set of reliable, tested, and proven methods alongside step-by-step guidance. This practical resource not only explores synthetic methodology, but also reaction mechanisms and applications in medicinal chemistry and drug discovery. The publication begins with an introductory chapter covering general principles and methodologies, nomenclature, and strategies of stereoselective synthesis. Next, it is divided into three parts: Part One: General Methods and Strategies Part Two: Stereoselective Synthesis by Bond Formation including C-C bond formation C-H bond formation C-O bond formation C-N bond formation Other C-heteroatom formation and other bond formation Part Three: Methods of Analysis and Chiral Separation References in every chapter serve as a gateway to the literature in the field. With this publication as their guide, chemists involved in the stereoselective synthesis of drugs and natural products now have a single, expertly edited source for all the methods they need.

Dissertation Abstracts International

Dissertation Abstracts International PDF Author:
Publisher:
ISBN:
Category : Dissertations, Academic
Languages : en
Pages : 782

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Book Description


Efficiency in Natural Product Total Synthesis

Efficiency in Natural Product Total Synthesis PDF Author: Pei-Qiang Huang
Publisher: John Wiley & Sons
ISBN: 1118940202
Category : Science
Languages : en
Pages : 512

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Book Description
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

Solid-Phase Organic Synthesis

Solid-Phase Organic Synthesis PDF Author: Kevin Burgess
Publisher: John Wiley & Sons
ISBN: 0471458457
Category : Science
Languages : en
Pages : 294

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Book Description
Solid-Phase Organic Synthesis Edited by Kevin Burgess, Texas A & M University Efficient, high-throughput chemistry is now the focus of many research laboratories. Solid-phase organic syntheses are central to many of these combinatorial and parallel screening methodologies. Consequently, they have been a major scientific theme of the 1990s and promise to remain prominent for the first part of the new millennium. Indeed, a bewildering number of papers have entered the literature on this topic; some report minor modifications enabling transformation of solution-phase methods to a solid support, while others report major innovations. Solid-Phase Organic Synthesis collects, highlights, and critiques some of the key developments in the field. Leading practitioners explain different perspectives on diverse aspects of the area. Specific topics covered include: * Syntheses of guanidines * Palladium-catalyzed C-C bond forming reactions * S_nAr reactions for the formation of heterocycles * Sequence-specific arylalkyne oligomers * Resin-supported capture agents and other reagents * Synthesis on pins * Monitoring of supported reactions using IR * Solid-phase syntheses of natural product derivatives Of related interest . Combinatorial Chemistry and Molecular Diversity in Drug Discovery Eric M. Gordon and James F. Kerwin 1998 (0-471-15518-7) 544 pp. Combinatorial Chemistry Synthesis and Application Stephen R. Wilson and Anthony W. Czarnik 1997 (0-471-12687-X) 288 pp.

Combinatorial Chemistry and Technology

Combinatorial Chemistry and Technology PDF Author: Stanislav Miertus
Publisher: CRC Press
ISBN: 9781420000566
Category : Science
Languages : en
Pages : 456

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Book Description
"Provides comprehensive coverage of the current combinatorial methodologies and technologies employed for the design, synthesis, and screening of molecular ""libraries."" Features assessments of computer-assisted approaches to guiding library synthesis. Designed to satisfy the demand to create, produce in high yield and purity, and rapidly screen huge numbers of molecules."

Combinatorial Chemistry

Combinatorial Chemistry PDF Author: Stephen R. Wilson
Publisher: John Wiley & Sons
ISBN: 9780471126874
Category : Medical
Languages : en
Pages : 288

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Book Description
The new time-saving revolution in drug discovery. Combinatorial chemistry, a method for synthesizing millions of chemical compounds much faster than usual, is becoming one of the most useful technical tools available to chemists and researchers working today. Using current advances in computer and laboratory techniques, combinatorial chemistry has freed professionals from the drudgery of piecemeal experimental work and opened new creative possibilities for experimentation. Combinatorial Chemistry: Synthesis and Application details critical aspects of the technique, featuring the work of some of the world's leading chemists, many of whom played a key role in its development. Including examples of both solution-phase and solid-phase approaches as well as the full complement of organic chemistry technologies currently available, the book describes: * Concepts and terms of combinatorial chemistry * Polymer-supported synthesis of organic compounds * Macro beads as microreactors * Solid-phase methods in combinatorial chemistry * Encoded combinatorial libraries, including Rf-encoding of synthesis beads * Strategies for combinatorial libraries of oligosaccharides * Combinatorial libraries of peptides, proteins, and antibodies using biological systems. While combinatorial chemistry originated in peptide chemistry, this volume has deliberately focused on nonpeptide organic applications, illustrating the technique's wide uses. Combinatorial Chemistry introduces organic, medicinal, and pharmaceutical chemists as well as biochemists to this exciting, cost-effective, and practical technique, which has unlocked creative potential for the next millennium.

Index Medicus

Index Medicus PDF Author:
Publisher:
ISBN:
Category : Medicine
Languages : en
Pages : 1780

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Book Description
Vols. for 1963- include as pt. 2 of the Jan. issue: Medical subject headings.

Organic Synthesis, Natural Products Isolation, Drug Design, Industry and the Environment

Organic Synthesis, Natural Products Isolation, Drug Design, Industry and the Environment PDF Author: Chhanda Mukhopadhyay
Publisher: Walter de Gruyter GmbH & Co KG
ISBN: 3111244075
Category : Science
Languages : en
Pages : 358

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Book Description
Over the years, applications of various non-conventional solvents diversified in various fields such as organic synthesis, natural products, drug design, pharmaceuticals, dyes and agrochemical industries. This book consists of nine chapters, which present recent advances and applications of various non-conventional solvents in organic transformations, drug design and bioremediation. Environmental impacts of non-conventional solvents and comparison between traditional solvents and non-conventional solvents are also discussed in this book.

Directory of Graduate Research

Directory of Graduate Research PDF Author:
Publisher:
ISBN:
Category : Chemistry
Languages : en
Pages : 1850

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Book Description
Faculties, publications and doctoral theses in departments or divisions of chemistry, chemical engineering, biochemistry and pharmaceutical and/or medicinal chemistry at universities in the United States and Canada.