Medicinal Chemistry plays an important role in drug discovery and development. One of the important steps in the process of drug discovery is synthesis of potent drug molecules using efficient, less time consuming, economical and environment friendly method. Another important component being purity and estimation of bulk and newly synthesized compounds using assay and other methods mentioned in the monographs. Both these components are very much helpful for the medicinal chemist in developing a novel moiety or to analyze the given compound. The medicinal chemists are primarily concerned with synthesis of organic molecules to be used as pharmaceuticals and the way these molecules interact in biological pathways. The synthesis involves a careful selection of a particular type of reaction, reagents, solvents, catalysts along with optimized reaction conditions. An understanding of organic reaction mechanism is essential otherwise, it is impossible to plan organic synthesis. The synthesis of pure drug molecules or compounds is important step in the process of drug discovery. This book provides a systematic, comprehensive knowledge about the various experiments of Medicinal Chemistry. The book provides the principle associated with each experiment, which enhances the understanding of reader. All the topics are explained in a very simple manner. The book provides detailed information about the assay and synthesis structure activity relationship procedure for many medicinal compounds, in such a manner that the reader should get a in depth knowledge about the medicinal chemistry of Medicinally active compounds All comments and suggestions will be received with gratitude. I am very much grateful to KLE Academy of Higher Education and Research, all my beloved teachers, parents, wife for their constant support and encouragement. Thanks to my daughters Ananya and Adhya, who are my stress relievers. I would like to express my heartfelt thanks to each and everyone who directly or indirectly helped me in compilation of this book Last but not the least I am very much thankful to all my students who are the inspiration for writing this book.