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Total Syntheses of Phleghenrines A and C

Xinpei Cai, Lei Li, Yecheng Wang, Jianhan Zhou, Mingji Dai

2023Organic Letters13 citationsDOIOpen Access PDF

Abstract

High Resolution Image Download MS PowerPoint Slide Herein, we report the total syntheses of phleghenrines A and C from commercially available starting materials in 7 and 8 steps, respectively. Notable steps include an inverse electron-demand Diels–Alder reaction between a masked o -benzoquinone and a N -protected enamine to prepare one key intermediate with a bicyclo[2.2.2]octenone core, a Büchner–Curtius–Schlotterbeck one-carbon insertion to expand the bicyclo[2.2.2]octenone to a bicyclo[3.2.2]nonenone, and Trauner’s modified 2-pyridone synthesis to install the 2-pyridone moiety.

Topics & Concepts

ChemistryBicyclic moleculeMoietyEnamineTotal synthesisCurtius rearrangementStereochemistryCombinatorial chemistryOrganic chemistryCatalysisTraditional and Medicinal Uses of AnnonaceaeChemical synthesis and alkaloidsAsymmetric Synthesis and Catalysis