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. 2020 Oct 16;22(20):7915-7919.
doi: 10.1021/acs.orglett.0c02837. Epub 2020 Sep 29.

Stereoselective Construction of γ-Lactams via Copper-Catalyzed Borylacylation

Alexa Torelli  1 , Andrew Whyte  1 , Iuliia Polishchuk  1 , Jonathan Bajohr  1 , Mark Lautens  1
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Stereoselective Construction of γ-Lactams via Copper-Catalyzed Borylacylation

Alexa Torelli et al. Org Lett. .

Abstract

A versatile and highly stereoselective borylative cyclization to generate polyfunctionalized γ-lactams has been developed. The stereoselective synthesis of these key ring systems is crucial due to their ubiquity in natural products. We report the diastero- and enantioselective construction of di- and trisubstituted γ-lactam cores, with examples containing an enantioenriched quaternary carbon.

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