In-flow Preparation and use of Diazo Compounds for Heterocycle Construction

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Heterocyclic compounds, ring structures in which one or more carbon atom is replaced by nitrogen, oxygen or sulfur are of vast importance. They account for well over half of all known organic compounds, and many classes of natural products, as well as a large majority of commercially important medicines, agrochemicals and reprographic materials, contain heterocyclic rings. Hence the synthesis and study of such compounds is a subject of immense significance, both in academia and industry. The commercial relevance of heterocyclic compounds is amply demonstrated by the list of best selling pharmaceuticals - for the year 2006, six of the top ten best sellers were nitrogen heterocycles with combined sales of $41 billion. This proposal, which has the full support of Pfizer, seeks support to develop efficient in-flow routes to heterocyclic compounds, based on the versatile chemistry of diazo compounds.