Stereoselective Synthesis Of Hexahydroimidazo[1,2-A]Quinolines Via S(N)2-Type Ring-Opening Hydroarylation-Hydroamination Cascade Cyclization Of Activated Aziridines With N-Propargylanilines
ORGANIC LETTERS(2020)
Abstract
A novel synthetic approach for the construction of 1,2,3,3a,4,5-hexahydroimidazo[1,2-a]quinolines in good yields (up to 75%) with excellent stereoselectivity (dr up to 94:6, ee up to >99%) under one-pot domino ring-opening cyclization (DROC) conditions has been developed. The DROC protocol proceeds through a Lewis acid catalyzed SN2-type ring-opening of activated aziridines with N-propargylanilines followed by intramolecular cyclization comprising concomitant hydroarylation and hydroamination steps in a domino fashion.
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Key words
stereoselective synthesis,activated aziridines,hydroarylation–hydroamination cascade cyclization,ring-opening
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