可扩展的抗肿瘤药物埃特替尼和卢比替丁的全合成。
A Scalable Total Synthesis of the Antitumor Agents Et-743 and Lurbinectedin.
机构信息
Interdisciplinary Center on Biology and Chemistry & State Key Laboratory of Bioorganic & Natural Products Chemistry, Center for Excellence in Molecular Synthesis, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032, China.
出版信息
Angew Chem Int Ed Engl. 2019 Mar 18;58(12):3972-3975. doi: 10.1002/anie.201900035. Epub 2019 Feb 14.
An efficient and scalable approach is described for the total synthesis of the marine natural product Et-743 and its derivative lubinectedin, which are valuable antitumor compounds. The method delivers 1.6 % overall yield in 26 total steps from Cbz-protected (S)-tyrosine. It features the use of a common advanced intermediate to create the right and left parts of these compounds, and a light-mediated remote C-H bond activation to assemble a benzo[1,3]dioxole-containing intermediate.
本文描述了一种高效、可扩展的方法，用于全合成海洋天然产物 Et-743 和其衍生物 lubinectedin，它们是有价值的抗肿瘤化合物。该方法从 Cbz 保护的 (S)-酪氨酸以 1.6%的总收率经过 26 步反应得到产物。该方法的特点是使用一个共同的高级中间体来构建这些化合物的左右部分，并通过光介导的远程 C-H 键活化来组装含苯并[1,3]二恶唑的中间体。
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