In the area of organic chemistry one major challenge we are currently faced with is how to assemble potentially useful molecules in new ways that generate molecular complexity and in sequences that are as efficient as possible. Our efforts in this regard, specifically for the preparation of amino containing compounds incorporating an aromatic ring, are described in this doctoral thesis. We discovered an interesting regioselectivity in an intramolecular Heck reaction, which we studied for a series of substrates that are unbiased in terms of the size of the newly formed ring, where very high levels of selectivity in relation to the new carbon-carbon bond are typically observed. DFT calculations were performed to attempt to shed light on the reaction sequence. This regioselective Heck reaction, combined with the reductive removal of the temporary amino-protecting group, allowed us to synthesize the Sceletium alkaloids: mesembrane, mesembranol and mesembrine.

"This book presents comprehensive accounts of the chemistry revolving around the sulphonamides. Sulfonamides are widely present in various drugs as a functional group and are a manmade synthetic drug. Hence, their extended research is a prerequisite for every practitioner of organic chemistry. Chapter 1 introduces the synthesis, reactivity, acidity, and pharmaceutical properties of the sulphonamides. It highlights the synthesis of biologically active sulphonamides, the study of their biological activity by QSAR method, and their medical applications. Chapter 2 deals with the classification of sulphonamides (i.e. acyclic and cyclic) and their structural activity relationship. It also describes the application of sulphonamides in pharmaceuticals as antimicrobial, anti-diabetic, anti-viral, anti-cancer, anti-inflammatory and anti-malarial agents. Chapter 3 reviews the synthetic attempts towards sulphonamide synthesis by employing the fixation of sulphur-dioxides. These approaches have been categorized into three parts: a) transition metal-catalyzed, b) employing Lewis acid, c) photocatalytic. Chapter 4 discusses the use of sulphonamides as potent organocatalysts, briefly describing how the mono- and C2-symmetric bis-sulfonamides act as efficient bifunctional and multifunctional organocatalysts in the enantioselective Michael addition of carbonyl compounds to alpha, beta-unsaturated compounds. Chapter 5 details the oxidative sulphonamidation of alkenes and dienes, which also direct the routes to the synthesis of numerous heterocycles and linear compounds. Special emphasis is given to the comparison of reactivity of triflamides, arenesulfonamides, and the deprotection of sulfonamides. Chapter 6 describes the therapeutic properties of sulphonamides, which are significantly increased by the presence of the metal ions and ligands. This complex generation provides the opportunity to exploit the unique properties of metal centers, such as multiple oxidation states, redox properties, a wide variety of coordination numbers, symmetries and structural patterns, which offer highly adaptable platforms for drug design. Chapter 7 provides an overview of the clinical applications of sulphonamides on the toxicity and pharmacokinetic aspects of various sulpha-drugs. The mechanism involved in the development of sulfonamide resistance is briefly discussed. Thus, this book summarizes important attempts undertaken by chemists and biologists worldwide in the area of sulphonamides. Most importantly, the book also correlates the structural activity relationship and the related biological activity of the sulphonamides, attracting both novice and experienced chemists across the globe"--

Sulfonamides are the commonly used antibiotics, which are used in the combination with other antibiotics to enhance their effect. They are absorbed in the intestine and are widely distributed into the tissues. Sulfonamides inhibit the growth of bacteria by reverse inhibition and block the cycle of folic acid synthesis while they are effective against only those bacteria which produce folic acid intracellular. This book discusses about the synthesis of sulfonamides their characterization with modern instruments and their importance. The antibacterial activity which increases their importance has also been discussed. This book is divided into different chapters which enables the readers to understand this book easily. Chapter 1 covers the general introduction of sulfonamides and techniques used for characterization and chapter 2 explains the previous scientific work done on sulfonamides. Chapter 3 contains the experimental work while chapter 4 discusses the results obtained. Figures, tables and schemes are used to make it easier for readers.

The number of available synthetic methods can be overwhelming. In order to create novel motifs and templates which confer new and potentially valuable drug-like properties, it is important to know which synthetic methodologies will give the best results. Similarly, which methodologies are used to progress potential drug candidates from leads through the development process? What are the current industrial research problems and how can they be resolved in an industrial setting? This book highlights key methods that have real impact in drug discovery and facilitate delivery of drug molecules. Synthetic Methods in Drug Discovery Volume 1 focuses on the hugely important area of transition metal mediated methods used in industry. Current methods of importance such as the Suzuki-Miyaura coupling, Buchwald-Hartwig couplings and CH activation are discussed. In addition, exciting emerging areas such as decarboxylative coupling, and the uses of iron and nickel in coupling reactions are also covered. This book provides both academic and industrial perspectives on some key reactions giving the reader an excellent overview of the techniques used in modern synthesis. Reaction types are conveniently framed in the context of their value to industry and the challenges and limitations of methodologies are discussed with relevant illustrative examples. Edited and authored by leading scientists from both academia and industry, this book will be a valuable reference for all chemists involved in drug discovery as well as postgraduate students in medicinal chemistry.