This dissertation is focused on the development of new methods to synthesize imidazoline scaffolds. The work discusses three new procedures developed in the Tepe lab to synthesize trans-oxazoline, trans-imidazoline, and 2,3-disubstituted quinoline scaffolds. In addition, a new guanidine base mediated diastereoselective aziridine synthesis is described in this work. These new synthetic methodologies provide access to compounds that were not easily accessible using previously described methods. Paths to oxazolines and imidazolines via modified Corey-Chaykovsky sulfur ylide chemistry are presented. Here, the sulfonium salts were treated with stable precursors of acyl imines and 1,3-diaza-1,3-butadiene intermediates, respectively, for the oxazoline and imidazoline syntheses. A modified Skraup-type reaction was employed to synthesize 2,3-disubstituted quinoline scaffolds where epoxides were treated with aromatic anilines under mild conditions in the presence of a Lewis acid.

Advances in Heterocyclic Chemistry, Volume 130, the latest release in this definitive series, provides a comprehensive review that combines descriptive synthetic chemistry and mechanistic insights to yield an understanding of how chemistry drives the preparation and useful properties of heterocyclic compounds. New chapters in this release include Recent Developments in the Radiolabeling of Heterocyclic Rings, Chemistry of Azetidines, Tricyclic Fused Bithiophenes and Related Analogues: Important Building Blocks for Conjugated Materials, Application of Electrochemical Methods in the Synthesis of Heterocyclic Compounds and Elucidation of Their Properties, Organometallic Complexes of Chelating Azines, and more. Considered the definitive serial in the field of heterocyclic chemistry Serves as the go-to reference for organic chemists, polymer chemists and many biological scientists Provides the latest comprehensive reviews as written by established authorities in the field Combines descriptive synthetic chemistry and mechanistic insights to enhance understanding on how chemistry drives the preparation and useful properties of heterocyclic compounds

Non-conventional synthetic methods may provide new and green methods for the preparation of bioactive heterocycles. These methods, such as microwave and ultrasound assisted synthesis, biocatalysis, photochemistry and electrosynthesis use less energy and may produce less waste to get the desired products when compared to traditional methods. This book explores the use of these methods when synthesizing various biologically relevant heterocyclic scaffolds. THE SERIES: GREEN BIOACTIVE HETEROCYCLES Heterocycles are a widely utilized group of molecules as they often contain bioactivity that is useful in drug development, agriculture, and other applications. However, their synthesis remains challenging with diffi cult to control functional groups. With a greater focus on sustainable synthesis practices, there is a need to develop greener synthetic methods for the synthesis of structurally diverse bioactive heterocyclic scaffolds. This series aims to do so, by collecting developments into common themes.

This book describes biosynthetic methods to synthesize heterocyclic compounds, offering a guide for the development of new drugs based on natural products. The authors explain the role of natural products in chemistry and their formation along with important analytical methods and techniques for working with heterocycles. • Covers methods and techniques: isotopic labelling, enzymes and mutants, and pathway identification • Provides a thorough resource of information specifically on heterocyclic natural products and their practical biosynthetic relevance • Explains the role of natural products in chemistry and their formation • Discusses gene cluster identification and the use of biogenetic engineering in pharmaceutical application

Green Synthetic Approaches for Biologically Relevant Heterocycles, Second Edition, Volume One: Advanced Synthetic Techniques reviews this significant group of organic compounds within the context of sustainable methods and processes, expanding on the first edition with fully updated coverage and a whole range of new chapters. Volume One explores advanced synthetic techniques, with each chapter presenting in-depth coverage of various green protocols for the synthesis of a wide variety of bioactive heterocycles that are classified on the basis of ring-size and/or the presence of heteroatoms. Techniques covered range from high pressure cycloaddition reactions and microwave irradiation to sustainable one-pot domino reactions. This updated edition is an essential resource on sustainable approaches for academic researchers, R&D professionals, and students working across medicinal, organic, natural product and green chemistry. Provides fully updated coverage of the field of greener heterocycle synthesis Includes new chapters on varied multicomponent reactions, alongside both traditional and novel approaches Presents information in an accessible style with an emphasis on sustainability

Enables researchers to fully realize the potential to discover new pharmaceuticals among heterocyclic compounds Integrating heterocyclic chemistry and drug discovery, this innovative text enables readers to understand how and why these two fields go hand in hand in the effective practice of medicinal chemistry. Contributions from international leaders in the field review more than 100 years of findings, explaining their relevance to contemporary drug discovery practice. Moreover, these authors have provided plenty of practical guidance and tips based on their own academic and industrial laboratory experience, helping readers avoid common pitfalls. Heterocyclic Chemistry in Drug Discovery is ideal for readers who want to fully realize the almost limitless potential to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features: Several case studies illustrating the role and application of 3, 4, 5, and 6+ heterocyclic ring systems in drug discovery Step-by-step descriptions of synthetic methods and practical techniques Examination of the physical properties for each heterocycle, including NMR data and quantum calculations Detailed explanations of the complexity and intricacies of reactivity and stability for each class of heterocycles Heterocyclic Chemistry in Drug Discovery is recommended as a textbook for organic and medicinal chemistry courses, particularly those emphasizing heterocyclic chemistry. The text also serves as a guide for medicinal and process chemists in the pharmaceutical industry, offering them new insights and new paths to explore for effective drug discovery.

This book covers the general properties of heterocyclic compounds and methods for their preparation to use in applications of green chemistry. Heterocyclic compounds are an important class of molecules in organic chemistry due to their presence in natural products and their use in pharmaceuticals and new materials. They also play a vital role in the metabolism of living cells. Heterocyclic compounds have a wide range of applications in agrochemicals, pharmaceuticals, veterinary products, etc. This research-oriented volume is ideal for readers who want to fully realize the almost limitless potential of heterocyclic compounds and to discover new and effective pharmaceuticals among heterocyclic compounds, the largest and most varied family of organic compounds. The book features several case studies and step-by-step descriptions of synthetic methods and practical techniques. It also serves as a guide for chemists, offering them new insights and new paths to explore for effective drug discovery.