Synthesis of the optically active key intermediate of FR901483 |
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Authors: | Shigeru Ieda Toshiyuki Kan Tohru Fukuyama |
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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 |
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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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