New Synthetic Strategies & Methods for Bioactive Aromatics and Heteroaromatics

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Importance of Organic Synthesis. Today, driving most advances in biology and material science is the science and art of making molecules - chemical synthesis. It allows for the practical supply of medicinals and materials that are difficult or impossible to acquire otherwise; it has profound consequences on human health (most therapeutic agents are synthesis-derived) and our standards of living (nanotubes, conducting polymers, smart phones, sensors). Fundamental discoveries in synthesis are at the heart of practical impact decades later, e.g. the 2010 Nobel and the 2014 Nobel (awarded for optical microscopy "allowing us to peer into the nanoworld" and track e.g. Alzheimer disease), is based on organic synthesis. The understanding of relationship of RNA and DNA is dependent on questions such as "why pentose and not hexose nucleic acids?" asked by organic chemists which will allow understanding of how life began (our prebiotic origins). Such basic questions must be answered before application in society, usually 20 years hence, can result. ***Our Research. We aim to discover methods for making molecules. Our focus is aromatic/heteroaromatic molecules since they make up 80% of current commercial drugs. Our major achievements are in the area of lithium organometallic chemistry and we have coupled these with modern catalytic transition metal chemistry. ***Our Impact. Aside from use on small scale in university labs, our fundamental research is now adapted worldwide in technologies for making marketable medicines and food protection agents, e.g. SustivaT (BMS, anti-AIDS), SilthiofamT (Monsanto, fungicide), LosartanT (BMS, anti-inflammatory), and very recently, a molecule (Merck) to inhibit an enzyme involved in pathological conditions, eg. anorexia, atherosclerosis, stroke. ***Our Future Goals. To continue in invention and enhancement of our focal themes of lithium and transition metal catalyzed reactions as platforms for new ways to make molecules which overcome today's critical problems of the traditional lengthy, uneconomical, and environmentally unacceptable routes of the past. (Imagine a chemical reaction at Resolute Bay temperatures; we do that and, remarkably, industry can use our -78 0C reaction but now we have discovered how to use much more reasonable temperatures.) In context of our areas of expertise, we will develop new technology, e.g. flow microreactor, to encourage the use of our basic research in pharma and biotech to make the medicinal agents for human health for the future.**