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Protecting-Group-Free Syntheses of ent-Kaurane Diterpenoids: [3+2+1] Cycloaddition/Cycloalkenylation Approach

Jin Wang, Benke Hong, Dachao Hu, Yuichiro Kadonaga, Ruyao Tang, Xiaoguang Lei*
J. Am. Chem. Soc. 2020, 142, 5, 2238-2243

The Yu's Rh-catalyzed [3+2+1] cycloaddition followed by a Pd-mediated 5-endo cycloalkenylation is shown to be a general and powerful approach for efficient construction of the tetracyclic core structure of ent-kaurane diterpenoids. The utility of this strategy was further demonstrated by concise and protecting-group-free total syntheses of ent-1α-hydroxykauran-12-one, 12-oxo-9,11-dehydrokaurene, and 12α-hydroxy-9,11-dehydrokaurene.

  • Jin Wang, Benke Hong, Dachao Hu, Yuichiro Kadonaga, Ruyao Tang, Xiaoguang Lei*
  • Journal of the American Chemical Society, Volume 142, Issue 5, 5 February 2020, Pages 2238-2243
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  • DOI: 10.1021/jacs.9b13722
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The Yu's Rh-catalyzed [3+2+1] cycloaddition followed by a Pd-mediated 5-endo cycloalkenylation is shown to be a general and powerful approach for efficient construction of the tetracyclic core structure of ent-kaurane diterpenoids. The utility of this strategy was further demonstrated by concise and protecting-group-free total syntheses of ent-1α-hydroxykauran-12-one, 12-oxo-9,11-dehydrokaurene, and 12α-hydroxy-9,11-dehydrokaurene.