Preface

Is asymmetric synthesis essential for modern drug discovery?

Asymmetric synthesis is essential for modern drug discovery, playing a pivotal role in developing safer and more effective therapeutics by enabling the selective production of a single enantiomer. Since many biological molecules, including drug targets, are chiral, the three-dimensional arrangement of atoms in a drug can significantly influence its biological activity, efficacy, and safety. Asymmetric synthesis offers the precise control necessary to produce the desired enantiomer, minimizing side effects and enhancing the therapeutic potential of drugs. This level of precision is fundamental in the era of precision medicine, where treatments are tailored to interact optimally with specific biological targets.

This book showcases cutting-edge experimental research on synthesizing various heterocyclic drugs using the principles of asymmetric synthesis, summarized across ten chapters. In Chapter 1, the authors have briefly discussed the basic principles of enantioselective synthesis, underscoring its critical importance in drug discovery and development, and highlighted the biological significance of chiral heterocycles, focusing on chiral amines and other related compounds. The asymmetric synthesis of bioactive chiral alkaloids and terpenoids has been discussed in Chapter 2.

Chapter 3 describes the synthesis of pharmacologically active spirooxindoles through asymmetric synthesis. A brief discussion of the chemistry of medicinally important chiral dihydropyrimidinones has been presented in Chapter 4.

In Chapter 5, the authors have a special focus on exploring the procedures for the asymmetric synthesis of biologically active piperazine and its derivatives. Chapter 6 deals with up-to-date improvement and novel trends in the green alternative synthesis of asymmetric oxazines. The chemistry of chiral triazoles and their biological significance have been discussed in Chapter 7. In Chapter 8, the authors have provided a comprehensive overview of the synthetic strategies and biological evaluations of chiral benzimidazole derivatives, underscoring their potential in pharmaceutical applications. Chapter 9, gives an insight into the chemistry of chiral pharmaceuticals, discussing the different classes of compounds that have been synthesized using asymmetric methods.

In conclusion, the goal of this book is to provide an overview of the research being conducted on the role of asymmetric synthesis in drug discovery. We hope the content will captivate aspiring researchers and inspire them to further explore novel chiral heterocycles for the treatment of various diseases. Additionally, we believe this book will be a valuable resource for researchers, academics, and industry professionals with a deep interest in this field.

We want to express our sincere admiration and gratitude to all the authors for their dedicated efforts in preparing the content of this book. We also extend our heartfelt thanks to the publishers and their team for efficiently handling the project at every stage. Lastly, we are deeply grateful to our family members for their unwavering support throughout this journey.