Advanced Synthetic Strategies toward Ginkgolide Diterpenoids: Total Synthesis of (±)-Ginkgolide C and Formal Syntheses of (±)-Ginkgolides A and B

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dc.contributor.author
Barriault, Louis
Hébert, Martin
Bellavance, Gabriel
dc.date.accepted
2025-06-18
dc.date.accessioned
2026-02-04T20:12:05Z
dc.date.available
2026-02-04T20:12:05Z
dc.date.issued
2025-06-25
dc.date.submitted
2025-04-26
dc.description.abstract - en
Ginkgolides are highly oxygenated diterpenes isolated from Ginkgo biloba that exhibit potent anti-inflammatory and neuroprotective properties. Their compact hexacyclic architecture—featuring multiple contiguous stereocenters, a spirocyclic core, and a rare tert-butyl group—presents a formidable challenge in synthetic organic chemistry. Herein, we report the first total synthesis of ginkgolide C (3), the most structurally complex member of this family, completed in 26 steps from commercially available materials. The synthesis is guided by a functional group–driven strategy that enables the convergent construction of the polycyclic core through key diastereoselective carbon–carbon bond formations, selective oxidations, and late-stage epoxide-opening lactonizations. In parallel, the formal syntheses of ginkgolides A (1) and B (2) were accomplished via interception of a late-stage intermediate in 17 steps, the shortest route to these targets reported to date. This work provides a unified synthetic platform for accessing the ginkgolide family and offers new opportunities for the synthesis and biological evaluation of related analogues.
dc.description.fosrcfull - en
This document is the unedited Author’s version of a Submitted Work that was subsequently accepted for publication in The Journal of Organic Chemistry, copyright © 2025 American Chemical Society after peer review. To access the final edited and published work see <a href="https://doi.org/10.1021/acs.joc.5c01012">https://doi.org/10.1021/acs.joc.5c01012</a>.
dc.description.fosrcfull-fosrctranslation - fr
Ce document est la version non éditée d'un travail soumis par l'auteur qui a été accepté pour publication dans The Journal of Organic Chemistry, droit d'auteur © 2025 American Chemical Society après évaluation par les pairs. Pour accéder au travail final édité et publié, voir <a href="https://doi.org/10.1021/acs.joc.5c01012">https://doi.org/10.1021/acs.joc.5c01012</a>.
dc.identifier.doi
https://doi.org/10.26434/chemrxiv-2025-ppm63
dc.identifier.issn
0022-3263
1520-6904
dc.identifier.uri
https://open-science.canada.ca/handle/123456789/4188
dc.language.iso
en
dc.publisher - en
American Chemical Society
dc.publisher - fr
American Chemical Society
dc.relation.isreplacedby
https://doi.org/10.1021/acs.joc.5c01012
dc.rights - en
Other
dc.rights - fr
Autre
dc.rights.openaccesslevel - en
Green
dc.rights.openaccesslevel - fr
Vert
dc.rights.uri - en
#description-element
dc.rights.uri - fr
#description-element
dc.subject - en
Chemistry
Health
Trees
dc.subject - fr
Chimie
Santé
Arbre
dc.subject.en - en
Chemistry
Health
Trees
dc.subject.fr - fr
Chimie
Santé
Arbre
dc.title - en
Advanced Synthetic Strategies toward Ginkgolide Diterpenoids: Total Synthesis of (±)-Ginkgolide C and Formal Syntheses of (±)-Ginkgolides A and B
dc.type - en
Submitted manuscript
dc.type - fr
Manuscrit soumis
local.article.journalissue
26
local.article.journaltitle - en
The Journal of Organic Chemistry
local.article.journalvolume
90
local.pagination
27 pages
local.peerreview - en
No
local.peerreview - fr
Non
local.requestdoi - en
No
local.requestdoi - fr
No
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