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Our research focuses on the development of catalytic asymmetric C-C bond-forming reactions with particular emphasis on high atom economy and their application to the synthesis of biologically significant compounds.Thus, the concept of asymmetric cooperative catalysis such as Lewis acid-Br(o)nsted base catalysis and Lewis acid-Lewis base catalysis plays the key role in our research paradigm.In this lecture, we report our recent achievement of catalytic asymmetric synthesis of biologically significant heterocyclic compounds such as Relenza, Ranirestat and Lipitol.