Stereoselective Total Synthesis of Eburnane-Type Alkaloids Enabled by Conformation-Directed Cyclization and Rearrangement
Controlling the cis C20/C21 relative stereochemistry remains an unsolved issue in the synthesis of eburnane-type indole alkaloids. Provided herein is a simple solution to this problem by developing a unified and diastereoselective synthesis of four representative members of this class of natural products, namely, eburnamonine, larutensine, terengganensine B, and melokhanine E. The synthesis features the following key steps: a) an a-iminol rearrangement transforming the 3-hydroxyindolenine into spiroindolin-3-one, b) a highly diastereoselective conformation-directed cyclization leading to the melokhanine skeleton with the desired C20/C21 cis stereochemistry, and c) either an aza pinacol or an unprecedented aaminoketone rearrangement converting spiroindolinone back into the indole skeleton.
Cite this item
Li, G., Piemontesi, C., Wang, Q., & Zhu, J. (2019). Stereoselective Total Synthesis of Eburnane-Type Alkaloids Enabled by Conformation-Directed Cyclization and Rearrangement. Angewandte Chemie International Edition, 58(9), 2870–2874. https://doi.org/10.1002/anie.201813920
Click Copy to copy the citation, or select the text manually.
2019
58
9
2870
2874
REVIEWED
EPFL
| Funder | Grant Number |
FNS | SNSF 20020-169077 |