埃克泰纳西丁的总合成 743
Atsushi Endo1, Arata Yanagisawa, Masanao Abe
1Graduate School of Pharmaceutical Sciences, The University of Tokyo, CREST, The Japan Science and Technology Cooperation (JST), 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033, Japan.
Journal of the American Chemical Society
|June 6, 2002
概括
已经成功地完成了强效抗瘤药物ecteinascidin 743的总合成. 这种复杂的分子是使用包括Ugi在内的关键反应来构建的.
科学领域:
- 有机化学 有机化学
- 药用化学 医学化学
- 药物发现 药物发现 药物发现
背景情况:
- 埃克泰纳西丁743是一种非常强大的抗瘤剂.
- 埃克泰纳西丁743的复杂结构构成了重要的合成挑战.
研究的目的:
- 为了实现ecteinascidin 743.的总合成
- 为这种有前途的抗癌化合物开发一种高效的合成途径.
主要方法:
- 乌吉的4中心,3组件 (4CC) 反应反应.
- 内部分子的赫克反应反应
- -化的循环化过程
- 酸诱导的分子内硫化物形成.
主要成果:
- 成功完成了ecteinascidin 743 (1) 的总合成.
- 合成途径有效地纳入了关键的结合形成反应.
结论:
- 完全合成ecteinascidin 743是可以实现的.
- 这项工作为进一步开发和模拟合成强效抗瘤剂提供了基础.
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