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Asymmetric Total Synthesis of Pedrolide

Wen Zhang, Peng-Cheng Yu, Chen-Yun Feng, Chuang‐Chuang Li

2024Journal of the American Chemical Society21 citationsDOI

Abstract

The asymmetric total synthesis of pedrolide (>200 mg) with an unprecedented [5-5-5-6-6-3] hexacyclic core (pedrolane) was achieved. Its unique bicyclo[2.2.1]heptane ring system was efficiently constructed via an enantioselective ene reaction of cyclopentadiene followed by a Wittig reaction, isomerization, and a diastereoselective intramolecular Diels-Alder reaction cascade. The highly oxygenated carane [6-3] ring system was synthesized via a ring-closing metathesis reaction followed by an unusual free carbene cyclopropanation. Furthermore, the 12 contiguous stereocenters of pedrolide were installed diastereoselectively.

Topics & Concepts

ChemistryTotal synthesisStereocenterEnantioselective synthesisIntramolecular forceCyclopropanationWittig reactionMetathesisHeptaneIsomerizationRing-closing metathesisRing (chemistry)StereochemistryCarbeneBicyclic moleculeSalt metathesis reactionCyclopentadieneOrganic chemistryCatalysisPolymerPolymerizationSynthetic Organic Chemistry MethodsBioactive Natural Diterpenoids ResearchAdvanced Synthetic Organic Chemistry
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