Total Synthesis of Dolastatin 10, An Antitumor Marine Peptide Containing Unusual Amino Acids.

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  • SHIOIRI Takayuki
    Department of Synthetic Organic Chemistry, Faculty of Pharmaceutical Sciences, Nagoya City University

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  • 異常アミノ酸を含有するペプチドの合成　ドラスタチン１０を例として
  • イジョウ アミノサン オ ガンユウスル ペプチド ノ ゴウセイ ドラスタチン

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Synthetic studies on dolastatin 10, an antitumor marine peptide containing unusual amino acids, are reviewed. Strategies for the synthesis of the C-terminal dolaphenine (Doe) are first described, and then the stereoselective synthesis of the two unusual amino acids, dolaproine (Dap) and dolaisoleuine (Dil), is discussed. Finally, the method for the construction of the whole molecule by assembling each amino acid unit is described.

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