Domino Reactions in Drug Discovery presents a concise selection of domino reactions employed in routes for the synthesis of pharmaceuticals, agrochemicals and the design of new drug candidates. These versatile reactions play an important and integral part in both the aesthetic appeal and functional aspects of strategic drug discovery, lending enhanced efficiency and synthetic versatility to pharmaceutical drug design. Due to their atom economy, these reactions are increasingly popular in the development of complex scaffolds and multifunctional derivatives aimed at the synthesis of new chemical entities and approved APIs across diverse therapeutic classes, including antidiabetics [DPP4 inhibitors], anticancer therapies and HIV integrase inhibitors.
- Features illustrated schemes with mechanisms, procedures and results
- Includes a compendium of Domino Name Reactions for drugs
- Provides a concise, comprehensive coverage of domino reactions in drug discovery, with a focus on sustainable practices
1. Introduction: Origin, Genesis and Relevance of Domino Reactions 2. Asymmetric Domino Reactions 3. Metal-Catalyzed Domino Reactions 4. Enzymatic Domino Processes 5. Heterocyclic Domino Reactions 6. Domino Reactions in the Synthesis of Target Molecules 7. Domino Name Reactions 8. Enzyme-catalysed Domino Reactions in Pharmaceutical Perspective 9. Case Studies of Coupled Name Reactions 10. Conventional route of synthesis as per product patent of drug 11. Comparison between DNR & conventional RoS [Route of Synthesis] 12. Applications of Domino Reactions in Chiral Drug Design 13. References & Suggested Readings: Literature Review including Patents
Dr. Shanta Bhar is a medicinal and computational scientist with 13 years of postdoctoral experience in designing and synthesizing new chemical entities and developing investigational new drug applications (NDAs) for diabetes, cancer, and inflammation with emphasis on pre-clinical small molecule drug discovery. Dr. Bhar specializes in domino reactions, computer-aided drug design (CADD), structure-based drug design (SBDD), and ligand-based drug design (LBDD), spanning the therapeutic areas of cancer, diabetes, and dengue. She works to aid therapeutic development by formulating concise, efficient and scalable synthetic strategies that integrate the versatility of domino reactions to generate complex derivatized scaffolds thus streamlining the process and economic viability of a drug from conception to approval. Dr. Bhar's current research is directed towards the synthesis of members of the epothilone family, a newer class of microtubule inhibitors, which is involved in the growth of solid tumors and VEGF [vascular endothelial growth factor] inhibitors, that affect the process of angiogenesis by reducing tumor size and tendency to metastasize. In both pharma research and academic pursuits, Dr. Bhar has laid out the roadmap and designed potential drug candidates. She has worked on lead optimization and design of retrosynthetic strategy, and has been exploring avenues to scale down complex syntheses or synthesis of complex drugs including chiral drugs. These include established pharmaceuticals, pre-clinical candidates, promising potential NCEs, and agrochemicals involving efficient utilization of Domino Reactions.