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Until the latter part of the 19th century, the majority of known drugs were either herbs or extracts of active ingredients from botanical sources. At this point, the world witnessed two major cornerstone achievements that laid the foundation of modern drug discovery and development: the emergence of pharmacology as a contemporary science through the work of Schmiedeberg (considered by many as the father of modern pharmacology) at the University of Strasbourg, andWoehler's landmark synthesis of urea from ammonium cyanate (the first synthesis of an 'organic' molecule from an 'inorganic' source) which heralded the birth of modern organic chemistry. Drug discovery has evolved from relying on luck, accident and serendipity to a complex endeavor that is at theinterface of several disciplines (e.g. pharmacology, biology, chemistry), and is built on the understanding of mechanisms and causes of diseases.This book is produced to celebrate the evolution of drug discovery and development. It will prove useful to synthetic organic chemists in both pharmaceutical industry and in academia, and can serve as a teaching tool to students who want to learn and understand the processes and challenges of drug discovery and development with real examples from top pharmaceutical companies. The chapters contain citations of a large number of valuable selected references to the primary literature. The bookhighlights the tireless efforts of discovery and process chemists, and their roles in the advancement of drug discovery and development.The chapters presented in this book are written by a selected group of outstanding, very accomplished medicinal and process chemists with noted experiences and diverse backgrounds, representing some of the top pharmaceutical companies. The chapters highlight examples of emerging concepts, new developments and challenges arising in the discovery of new drug candidates and the development of new practical synthetic chemistry processes to produce these drug candidates on large scale. The discoveryof each drug or drug candidate is presented by the discovery chemist(s) and the process chemist(s) who developed the drug. These writing teams describe the drug's development to give the reader a complete story of drug discovery and development.