Several novel multicomponent assembly processes have been developed for the preparation of a diverse array of complex heterocyclic systems from relatively simple starting materials. These studies resulted in the discovery of a new quinazolone forming reaction, which was applied to the one-step synthesis of the quinazolinocarboline alkaloid rutaecarpine. Biological screening of these complex heterocycles culminated in the identification of a potent sigma-2 receptor ligand. A novel N-acyliminium ion mediated cascade reaction was employed for the concise synthesis of (±)-actinophyllic acid. The completion of the synthesis relied on the development of a reaction sequence that avoided a potentially detrimental fragmentation process. Furthermore, several anti-cancer compounds were identified through a diverted total synthesis approach.

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.

Has the concept of Diversity Oriented Synthesis remained unchanged over these two decades, or do we observe improvements or deviations from the original guidelines drawn by the pioneers? The aim of this Research Topic is to collect contributions on the state-of-the-art and progress of Diversity Oriented Synthesis, and to foresee its shape in the next decade.

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.

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.

Filling the need for a ready reference that reflects the vast developments in this field, this book presents everything from fundamentals, applications, various reaction types, and technical applications. Edited by rising stars in the scientific community, the text focuses solely on visible light photocatalysis in the context of organic chemistry. This primarily entails photoinduced electron transfer and energy transfer chemistry sensitized by polypyridyl complexes, yet also includes the use of organic dyes and heterogeneous catalysts. A valuable resource to the synthetic organic community, polymer and medicinal chemists, as well as industry professionals.