GOALI: C-H Bond Activation and Functionalization Methods for Medicinal and Process Chemistry

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This GOALI project will continue work to establish Ir-catalyzed C-H borylations as an efficient route to aryl and heteroaryl boronic esters and allied molecules. While boronic esters serve as useful building blocks for pharmaceuticals, materials, and other valuable compounds, their preparation often requires the employment of haolgenated aromatics. This reliance on halogenated starting materials raises environmental concerns and limits the availability of many potentially useful boronic esters. Studies aimed at developing new and orthogonal strategies for the direct borylation and further functionalization of pharmaceutically relevant molecules will be undertaken. Screening of diverse substrates and catalysts/reagent combinations will be used to develop mechanistic models of these reactions and to expand the chemical space in which these reactions can operate. With this award, the Chemical Synthesis Program is supporting the research of Professors Robert E. Maleczka, Jr. and Milton R. Smith, III of the Department of Chemistry at Michigan State University, who will be working in collaboration with Dr. Yongkui Sun of Merck and in consultation with the American Chemical Society-Green Chemistry Institute's Pharmaceutical Roundtable. Professor Smith and Maleczka's collaborative research efforts revolve around the development of green chemistry methods for the formation and subsequent reaction of C-B bonds. Successful development of these reactions will positively impact discovery and process development in the pharmaceutical and other high tech industries. In addition, the academic research groups at Michigan State University will be exposed to the technical problems of concern at a major pharmaceutical company.