Graduate School of Pharmaceutical Sciences, Kyoto University, Yoshida, Sakyo-ku, Kyoto 606-8501, Japan.
J Org Chem. 2010 Jul 16;75(14):4876-9. doi: 10.1021/jo100788j.
Synthesis of the pentacyclic core of ecteinascidin 743 is described. This synthesis features concise construction of the diazabicyclo[3.3.1]nonane skeleton using gold(I)-catalyzed one-pot keto amide formation, acid-promoted enamide formation, and oxidative Friedel-Crafts cyclization as the key steps.
本文描述了埃替拉西宾 743 五环核心的合成。该合成的关键步骤包括使用金(I)催化的一锅法酮酰胺形成、酸促进的烯酰胺形成和氧化 Friedel-Crafts 环化,简洁地构建了二氮杂双环[3.3.1]壬烷骨架。