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This book reviews diversity-oriented synthesis (DOS), a leading and dynamic area in organic chemistry and drug discovery. It first covers key chemical methods for the generation of small molecules according to DOS principles as well as important classes of molecules generated through DOS approaches. The concept of diversity-oriented synthesis is then expanded to the description of chemical libraries. The book also examines modern approaches for screening DOS libraries and concludes with significant applications of DOS libraries and small molecules in the fields of drug discovery and chemical biology.
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