Synthetic Studies on Ecteinascidin 743

DOI
  • Imai Takahiro
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Nakata Hiyoku
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Yokoshima Satoshi
    Graduate School of Pharmaceutical Sciences, The University of Tokyo
  • Kan Toshiyuki
    School of Pharmaceutical Sciences, University of Shizuoka
  • Fukuyama Tohru
    Graduate School of Pharmaceutical Sciences, The University of Tokyo

Bibliographic Information

Other Title
  • エクチナサイジン743の合成研究

Description

Ecteinascidin 743 (ET 743) is an extremely potent antitumor agent isolated from a marine tunicate, Ecteinascida turbinate. ET 743 is currently undergoing phase II/III clinical trials in Europe and the United States. The novel structural features, poor availability from the natural sources, and the unique mechanism of action have made ET 743 a very attractive target for synthetic chemists. To date, total syntheses have been completed by Corey, Danishefsky, Zhu, and ourselves. We report herein a formal total synthesis of ET 743, featuring a regio- and stereoselective Pictet-Spengler reaction to afford the tetahydroisoquinoline and a diastereoselective Mannich-type reaction of the iminolactone. We have succeeded in the efficient construction of the bicyclo[3.3.1] skeleton from the Mannich-type reaction product.

Journal

Keywords

Details 詳細情報について

  • CRID
    1390282680610237568
  • NII Article ID
    130006995642
  • DOI
    10.14895/hannou.33.0.66.0
  • Text Lang
    ja
  • Data Source
    • JaLC
    • CiNii Articles
  • Abstract License Flag
    Disallowed

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