This book gives an overview of the current state of the art of combinatorial organic synthesis. While the main focus is on multicomponent and multigeneration strategies using polymeric supports, there is also a Chapter on solution strategies using polymer-grafted reagents which allow minimisation of work-up procedures. Some of the most important strategies and tools are presented and summarised, with an explanation of the pivotal role of organic synthesis in the creation of diversity.

The words "Combinatorial Chemistry" have different meanings to different people, ranging from split and mix strategies to parallel synthesis using robots, and embracing the whole range of preparative chemistry from organic molecules, to catalyst ligands, and even inorganic solids. All of these activities have in common an attempt to expand the diversity of structure available to the chemist as well as the access to this diversity, permitting the discovery of new and valuable biological acid material properties. In this outstanding survey of combinatorial organic chemistry, the authors, Obrecht who has established a new combinatorial chemistry company called Polyphor, and Villalgardo have brought together the literature, including that from 1998, and have concisely analysed the applications and achievements of this new field. This work will be of value to all chemists engaged in preparative work, both in industry and academe.

The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.

This book gives an overview of the current state of the art of combinatorial organic synthesis. While the main focus is on multicomponent and multigeneration strategies using polymeric supports, there is also a Chapter on solution strategies using polymer-grafted reagents which allow minimisation of work-up procedures. Some of the most important strategies and tools are presented and summarised, with an explanation of the pivotal role of organic synthesis in the creation of diversity.

With the explosion of combinatorial solid-phase methods, access to information has become one of the main barriers facing a synthetic chemist who is contemplating a combinatorial approach to a medicinal chemistry problem. The Combinatorial Index is an answer to that problem. This compendium of methods from the primary literature provides quick and convenient access to reliable synthetic transformations as well as information on linkers and analytical methods. Each synthetic procedure is preceded by a section entitled"Points of Interest,"which highlights the strengths and weaknesses of the various studies. The index also covers the use of solution-based synthesis for the generation of molecular diversity. - Organized for rapid retrieval of published information on classes of synthetic transformations, linkers, and analytical methods - Serves as a laboratory manual for bench chemists - Includes a chapter on linkers to assist in choice of linking strategy - Discusses strengths and limitations of the various methods - Contains a structural index showing functional group transformations in solid-phase synthesis

Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinato

Biphasic Chemistry and The Solvent Case examines recent improvements in reaction conditions, in order to affirm the role of chemistry in the sustainable field. This book shows that those who work within the chemistry industry support limits for the use of toxic or flammable solvents, since it reduces the purifications to simple filtrations. Thanks to commercial scavengers, solid phase syntheses are now available to all. Fluorine biphasic catalysis enables extremely efficient catalyst recycling and has a high applicability potential at the industrial level. This book also reviews the many studies that have shown that water is a solvent of choice for most synthetic reactions. Particular traits can be obtained and the effects on thermodynamics make it possible to operate at lower temperatures, thereby achieving energy savings. Finally the great diversity of application of the reactions without solvents is illustrated.