Alternatives to palladium catalysis for the elaboration of nitrogen heterocycles

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Prior to the development of synthetic organic chemistry, organic compounds were accessible only through natural biological processes. With the advancement of the chemical sciences especially since the 1950s, molecules of great complexity can now be readily synthesized providing medicines and crop protection agents for the benefit of humankind. Currently, palladium-catalyzed bond forming reactions are one of the most popular techniques used by synthetic chemists to prepare desired organic compounds, including pharmaceutically important heteroaromatic derivatives which constitute 80% of today's antibiotics, anticancer, anti-inflammatory and other medicinal agents. Although palladium-mediated methods have become a widely used synthetic tool, palladium metal is expensive and can be difficult to remove from the synthetic steps involved in drug preparation. Through this proposal, we aim to find alternative methods to synthesize heteroaromatic compounds for their use in the pharmaceutical and chemical industry. Previous methods discovered and developed in our laboratories are being used by the pharmaceutical industry (e.g. Monsanto, Pfizer, BMS, Merck) for the multikilogram commercial production of drugs, agrochemicals, and other commodity chemicals. This research proposal aims to help produce methods to make less expensive drugs and hence provide health and economic benefits to Canadians and, in the process, train highly qualified workers for the Canadian labour market.