Organocatalytic Asymmetric Dearomative Spirocyclization/Oxa-Michael Addition Sequence: Synthesis of Polycyclic Tetralones

Org Lett. 2024 Apr 19;26(15):3179-3183. doi: 10.1021/acs.orglett.4c00781. Epub 2024 Apr 3.

Abstract

Herein, an organocatalytic asymmetric dearomative spirocyclization/oxa-Michael addition sequence with a newly designed substrate having two naphthol motifs has been developed. The reaction proceeds through in situ chiral vinylidene ortho-quinone methide (VQM) intermediate formation, dearomative spirocyclization of naphthol, and an oxa-Michael addition reaction. The densely functionalized tetralone products were formed in high yields with high diastereo- and enantioselectivities.