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Direct cyclopropanation of activated N-heteroarenes <i>via</i> site- and stereoselective dearomative reactions

Jiyoun Lee, Donguk Ko, Hyun-Ju Park, Eun Jeong Yoo

2020Chemical Science38 citationsDOIOpen Access PDF

Abstract

the dearomative addition of sulfur ylides to activated N-heteroarenes. A series of biologically significant molecular skeletons was obtained by the direct cyclopropanation of quinolinium zwitterions. Furthermore, a straightforward synthetic route to optically enriched cyclopropane-fused heterocycles was developed using sulfur ylides as chiral nucleophiles in the 1,4-dearomative reaction.

Topics & Concepts

CyclopropanationStereoselectivityChemistryMedicinal chemistryCombinatorial chemistryStereochemistryCatalysisOrganic chemistryCyclopropane Reaction MechanismsCatalytic Cross-Coupling ReactionsAsymmetric Synthesis and Catalysis