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Author: Nasim Esmati
Publisher:
ISBN:
Category : Bioactive compounds
Languages : en
Pages : 164
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Book Description
Generating molecular complexity and molecular diversity in a simple and rapid process has become one of the most challenging yet increasingly popular concepts in organic chemistry over the past few years. Taking this into consideration, the design of various types of chemical building blocks to prepare a small library of natural products or biological active molecules has become a significant objective. To fulfill these objectives, one can take advantage of multi component reactions (MCRs), in which three or more starting materials react to form a single product, where basically all or most of the atoms contribute to the newly formed product. MCRs have the ability of combining commercially available or readily accessible multiple starting materials with a variety of functionalities in one-step and then invoking post modification steps, like various kinds of ring formations and rearrangements. The experimental simplicity of one-pot procedures can give access to a diverse library of compounds rapidly, which makes the procedure more advantageous over multistep syntheses. All these important factors provide the opportunity to work on combinatorial chemistry which counts as a fundamental phenomenon in finding novel molecules for medicinal chemistry. The development and application of multicomponent reactions have attracted much attention in recent years since they are very useful synthetic tools for synthesize of potential pharmaceutically bioactive scaffolds. Post modified transformation of MCRs have great importance for accessing the synthetic building blocks for complex natural products and their analogues to investigate their possibility in treating various diseases. In the first project, we attempted the synthesis and biological study of Derivatives of the herbicide thaxtomin, through Ugi/keto-amide cyclization and Ugi/Dess-Martin/keto-amide cyclization sequences. The Ugi reaction was utilized with 3-nitrobenzaldehyde, indole-3-carboxaldehydes, phenyl lactic acid, methylamine, and methyl isocyanide to prepare dipeptides which then underwent oxidation to a- ketoamide intermediates followed by subsequent alkaline mediated keto-amide cyclization to syn and anti hemiaminal DKPs. In the second project, we reported a one-pot, two-step, total synthesis of naturally occurring Xenortides A, B, C and D, (Xens A-D) isolated from the bacterium Xenorhabdus nematophila, and an entire complimentary set of stereoisomers. The syntheses were accomplished utilizing an isocyanide-based Ugi 4-CR followed by facile N-Boc deprotection. The reaction sequence takes advantage of the chiral pool of N-Boc protected amino acids (L-Leu/Val and D-Leu/Val) with aryl isocyanides, phenyl acetaldehyde and methylamine giving the desired Xens A-D and all subsequent stereoisomers. Moreover, this focused library of naturally occurring Xens A-D and their subsequent stereoisomers were screened for cytotoxicity against a panel of epithelial cancer cell lines as well as normal cell lines.
Author: Nasim Esmati
Publisher:
ISBN:
Category : Bioactive compounds
Languages : en
Pages : 164
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Book Description
Generating molecular complexity and molecular diversity in a simple and rapid process has become one of the most challenging yet increasingly popular concepts in organic chemistry over the past few years. Taking this into consideration, the design of various types of chemical building blocks to prepare a small library of natural products or biological active molecules has become a significant objective. To fulfill these objectives, one can take advantage of multi component reactions (MCRs), in which three or more starting materials react to form a single product, where basically all or most of the atoms contribute to the newly formed product. MCRs have the ability of combining commercially available or readily accessible multiple starting materials with a variety of functionalities in one-step and then invoking post modification steps, like various kinds of ring formations and rearrangements. The experimental simplicity of one-pot procedures can give access to a diverse library of compounds rapidly, which makes the procedure more advantageous over multistep syntheses. All these important factors provide the opportunity to work on combinatorial chemistry which counts as a fundamental phenomenon in finding novel molecules for medicinal chemistry. The development and application of multicomponent reactions have attracted much attention in recent years since they are very useful synthetic tools for synthesize of potential pharmaceutically bioactive scaffolds. Post modified transformation of MCRs have great importance for accessing the synthetic building blocks for complex natural products and their analogues to investigate their possibility in treating various diseases. In the first project, we attempted the synthesis and biological study of Derivatives of the herbicide thaxtomin, through Ugi/keto-amide cyclization and Ugi/Dess-Martin/keto-amide cyclization sequences. The Ugi reaction was utilized with 3-nitrobenzaldehyde, indole-3-carboxaldehydes, phenyl lactic acid, methylamine, and methyl isocyanide to prepare dipeptides which then underwent oxidation to a- ketoamide intermediates followed by subsequent alkaline mediated keto-amide cyclization to syn and anti hemiaminal DKPs. In the second project, we reported a one-pot, two-step, total synthesis of naturally occurring Xenortides A, B, C and D, (Xens A-D) isolated from the bacterium Xenorhabdus nematophila, and an entire complimentary set of stereoisomers. The syntheses were accomplished utilizing an isocyanide-based Ugi 4-CR followed by facile N-Boc deprotection. The reaction sequence takes advantage of the chiral pool of N-Boc protected amino acids (L-Leu/Val and D-Leu/Val) with aryl isocyanides, phenyl acetaldehyde and methylamine giving the desired Xens A-D and all subsequent stereoisomers. Moreover, this focused library of naturally occurring Xens A-D and their subsequent stereoisomers were screened for cytotoxicity against a panel of epithelial cancer cell lines as well as normal cell lines.
Author: Jieping Zhu
Publisher: John Wiley & Sons
ISBN: 3527332375
Category : Science
Languages : en
Pages : 512
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Book Description
Comprehensive and up-to-date, this book focuses on the latest advances in the field, such as newly developed techniques, more environmentally benign processes, broadened scopes, and completely novel MCRs. In addition to carbene-promoted MCRs and frequently applied metal-catalyzed MCRs, it also covers recently developed catalytic enantioselective variants as well as MCR in drug discovery and for the synthesis of heterocyclic molecules and macrocycles. Edited by the leading experts and with a list of authors reading like a "who's who" in multicomponent reaction chemistry, this is definitely a must-have for every synthetic organic chemist as well as medicinal chemists working in academia and pharmaceutical companies.
Author: Raquel P. Herrera
Publisher: John Wiley & Sons
ISBN: 1118863976
Category : Science
Languages : en
Pages : 523
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Book Description
Addressing a dynamic aspect of organic chemistry, this book describes synthetic strategies and applications for multicomponent reactions – including key routes for synthesizing complex molecules. • Illustrates the crucial role and the important utility of multicomponent reactions (MCRs) to organic syntheses • Compiles novel and efficient synthetic multicomponent procedures to give readers a complete picture of this class of organic reactions • Helps readers to design efficient and practical transformations using multicomponent reaction strategies • Describes reaction background, applications to synthesize complex molecules and drugs, and reaction mechanisms
Author: Alaa Zidan
Publisher:
ISBN:
Category :
Languages : en
Pages : 0
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Book Description
Author: Erik Van der Eycken
Publisher: John Wiley & Sons
ISBN: 3527349081
Category : Science
Languages : en
Pages : 626
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Book Description
Presents a wide-ranging overview of essential topics and recent advances in MCR chemistry Heterocycles are a central component in natural product chemistry, pharmaceuticals, agrochemicals, and material science. New synthetic methodologies integrating the sequencing of multicomponent reactions (MCRs) are today being used for the rapid synthesis of diversified heterocycles in just one step. Multicomponent Reactions towards Heterocycles presents an up-to-date summary MCR chemistry with a focus on the conjugation between modern synthetic methodologies and MCRs. Featuring contributions by leaders in the field, this comprehensive resource highlights applications of MCRs in natural products and intermediate synthesis, discusses current trends and future prospects in MCR chemistry, outlines novel multicomponent procedures, and more. The authors provide the practical information required for designing new reaction strategies and mechanisms, covering topics including MCR-based green synthetic methods, cyclization and cycloaddition reactions, heterocycle multicomponent syntheses in a continuous flow, catalytic alkynoyl generation, MCR synthesis of saturated heterocycles, and C–H functionalization and multicomponent reactions. Provides a thorough overview of heterocycles as input in multicomponent reactions Discusses recent advances in the field of MCR chemistry and progress in the synthesis and functionalization of heterocycles Demonstrates the use of MCRs to simplify synthetic design and achieve complexity and diversity in novel bioactive molecules Highlights examples of multicomponent polymerizations, target-oriented synthesis, and applications of MCR in medicinal chemistry Explains the methodology of using on-resin MCRs to produce heterocycle compounds Illustrating the key role of MCRs towards heterocycles in natural product synthesis, drug discovery, organic synthesis, and other applications, Multicomponent Reactions towards Heterocycles is required reading for synthetic chemists in academia and industry alike.
Author: K. L. Ameta
Publisher: Springer
ISBN: 8132218507
Category : Science
Languages : en
Pages : 418
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Book Description
The book presents a succinct summary of methods for the synthesis and biological activities of various different-sized bioactive heterocycles using different green chemistry synthetic methodologies, like microwave, ultrasonic, water mediated, ionic liquids, etc. The book also provides an insight of how green chemistry techniques are specific to the bioactive heterocyclic compounds.
Author: Jonathan G. Rudick
Publisher: Frontiers Media SA
ISBN: 2889634841
Category :
Languages : en
Pages : 100
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Book Description
This eBook is a collection of articles from a Frontiers Research Topic. Frontiers Research Topics are very popular trademarks of the Frontiers Journals Series: they are collections of at least ten articles, all centered on a particular subject. With their unique mix of varied contributions from Original Research to Review Articles, Frontiers Research Topics unify the most influential researchers, the latest key findings and historical advances in a hot research area! Find out more on how to host your own Frontiers Research Topic or contribute to one as an author by contacting the Frontiers Editorial Office: frontiersin.org/about/contact.
Author: Maurizio Benaglia
Publisher: John Wiley & Sons
ISBN: 9780470682012
Category : Science
Languages : en
Pages : 500
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Book Description
Recoverable and Recyclable Catalysts There is continued pressure on chemical and pharmaceutical industries to reduce chemical waste and improve the selectivity and efficiency of synthetic processes. The need to implement green chemistry principles is a driving force towards the development of recoverable and recyclable catalysts. The design and synthesis of recoverable catalysts is a highly challenging interdisciplinary field combining chemistry, materials science engineering with economic and environmental objectives. Drawing on international research and highlighting recent developments, this book serves as a practical guide for both experts and newcomers to the field. Topics covered include: An introduction to the principles of catalyst recovery and recycling Catalysts on insoluble and soluble support materials Thermomorphic catalysts, self-supported catalysts and perfluorous catalytic systems The development of reusable organic catalysts Continuous flow and membrane reactors Each chapter combines principles with practical information on the synthesis of catalysts and strategies for catalyst recovery. The book concludes with a comparison of different catalytic systems, using case studies to illustrate the key features of each approach. Recoverable and Recyclable Catalysts is a valuable reference source for academic researchers and professionals from a range of pharmaceutical and chemical industries, particularly those working in catalysis, organic synthesis and sustainable chemistry.
Author: Selcan Karakuş
Publisher: BoD – Books on Demand
ISBN: 1838800018
Category : Science
Languages : en
Pages : 162
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Book Description
This book was written by authors in the field of ultrasound-assited synthesis and their applications. Among others, some of the topics covered are: ultrasound-assited synthesis of metal/metal oxide nanoparticles, graphene nanosheets, and ultrasound applications. In this book, authors focused on recent studies, applications, and new technological developments on fundamental properties of the ultrasound process.
Author: Dr Stefano Protti
Publisher: Royal Society of Chemistry
ISBN: 1839162031
Category : Science
Languages : en
Pages : 602
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Book Description
Recent years have seen huge growth in the area of sustainable chemistry. In order to meet the chemical needs of the global population whilst minimising impacts on health and the environment it is essential to keep reconsidering and improving synthetic processes. Sustainable Organic Synthesis is a comprehensive collection of contributions, provided by specialists in Green Chemistry, covering topics ranging from catalytic approaches to benign and alternative reaction media, and innovative and more efficient technologies.