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Total Synthesis of (−)-Mitrephorone A Enabled by Stereoselective Nitrile Oxide Cycloaddition and Tetrasubstituted Olefin Synthesis

M. Schneider, Matthieu J. R. Richter, Erick M. Carreira

2020Journal of the American Chemical Society47 citationsDOIOpen Access PDF

Abstract

A highly enantioselective and diastereoselective total synthesis of the diterpenoid (-)-mitrephorone A is presented. Key to the synthesis are stereocontrolled 1,4-semihydrogenation of a 1,3-diene to a tetrasubstituted double bond, enzyme-catalyzed malonate desymmetrization, and highly diastereoselective nitrile oxide cycloaddition. The streamlined strategy is a considerable improvement to those reported earlier in terms of diastereo- and enantioselectivity. For the first time, the combination of modern Pd-cross-coupling with Cr-catalyzed reduction allows for rapid access to tetrasubstituted olefins with full stereocontrol.

Topics & Concepts

ChemistryDesymmetrizationNitrileEnantioselective synthesisCycloadditionTotal synthesisOlefin fiberStereoselectivityMalonateDouble bondStereochemistryCombinatorial chemistryDieneCatalysisOrganic chemistryNatural rubberSynthetic Organic Chemistry MethodsAdvanced Synthetic Organic ChemistryTraditional and Medicinal Uses of Annonaceae
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