Volume 110, Issue 1-2 pp. 89-92
Zuschrift

Totalsynthese von Epothilon E und seitenkettenmodifizierten Epothilon-Analoga durch Stille-Kupplung

K. C. Nicolaou

K. C. Nicolaou

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road „La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469

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Yun He

Yun He

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road „La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469

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Frank Roschangar

Frank Roschangar

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road „La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469

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N. Paul King

N. Paul King

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road „La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469

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Dionisios Vourloumis

Dionisios Vourloumis

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road „La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469

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Tianhu Li

Tianhu Li

Department of Chemistry and The Skaggs Institute for Chemical Biology, The Scripps Research Institute, 10550 North Torrey Pines Road „La Jolla, CA 92037, USA, (und) Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093, USA, Telefax: Int.+619/784-2469

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Abstract

Ringschluß durch Olefinmetathese (siehe unten, a), Abspaltung der Schutzgruppe (b), Stille-Kupplung (c) und die abschließende Epoxidierung (d) sind die wesentlichen Schritte der ersten Totalsynthese des natürlich vorkommenden Epothilons E 1. Ausgehend von dem Produkt der Olefinmetathese, einer sehr fortgeschrittenen Zwischenstufe, ist eine Fülle von Epothilon-E-Analoga mit unterschiedlichen aromatischen Resten in der Seitenkette zugänglich. TBS = tBuMe2Si.

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