Journal
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
Volume 58, Issue 12, Pages 3972-3975Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201900035
Keywords
antitumor agents; C-H bond activation; cyclization; marine natural products; total synthesis
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Funding
- Chinese Academy of Sciences (Strategic Priority Research Program) [XDB20020200, QYZDJ-SSW-SLH029]
- National Natural Science Foundation of China [21621002, 21831009]
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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.
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