Diastereo- and Enantioselective Synthesis of Functionalized Dihydropyrans via an Organocatalytic Claisen Rearrangement/Oxa-Michael Addition Tandem Sequence

Org Lett. 2023 Sep 1;25(34):6434-6439. doi: 10.1021/acs.orglett.3c02461. Epub 2023 Aug 22.

Abstract

A straightforward diastereo- and enantioselective Claisen rearrangement/oxa-Michael addition tandem sequence with a cinchona squaramide catalyst was described, which afforded a practical and atom-economical approach to access a range of valuable dihydropyrans in good to excellent yields with excellent stereoselectivities. The organo-bifunctional catalyst played a key role in enhancing stereoselectivity in this asymmetric tandem sequence. Moreover, the asymmetric catalytic sequential processes of the hydroalkoxylation/Claisen rearrangement/cyclization sequence and Claisen rearrangement/aza-Michael addition tandem sequence have also been afforded good yields and moderate stereoselectivities.