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Synthesis of the optically active key intermediate of FR901483
Authors:Shigeru Ieda  Toshiyuki Kan  Tohru Fukuyama
Affiliation:a Graduate School of Pharmaceutical Science, University of Tokyo 7-3-1 Hongo, Bunkyo-ku 113-0033, Japan
b School of Pharmaceutical Sciences, University of Shizuoka and Global COE Program, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan
Abstract:Efficient synthesis of the tricyclic key intermediate 2 for (−)-FR901483 1 was accomplished. The precursor of the intramolecular aldol reaction 4b is constructed by the Ugi 4CC reaction and subsequent intramolecular Dieckmann condensation. This approach allows a fully stereocontrolled total synthesis of (−)-FR901483, which would provide various derivatives.
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