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Synthesis of Tamiflu (Oseltamivir)
H. Ishikawa, T. Suzuki, Y. Hayashi*
Tokyo University of Science, Japan
22 June 2009 (online)
A remarkably short and efficient synthesis of (-)-oseltamivir is reported featuring an organocatalytic Michael addition (100% yield) as the first step. The sequence requires only three one-pot operations and proceeds in 57% overall yield from the nitroalkene B. The three one-pot operations involved the conversions of (1) B to G, (2) G to H and (3) H to oseltamivir.