Type 1 ring-opening reactions of cyclopropanated 7-oxabenzonorbornadienes with organocuprates

Org Lett. 2014 Mar 21;16(6):1776-9. doi: 10.1021/ol5004737. Epub 2014 Mar 11.

Abstract

For the first time, nucleophilic ring-openings of cyclopropanated 7-oxabenzonorbornadiene were investigated, providing a novel approach to the preparation of 2-methyl-1,2-dihydronaphthalen-1-ols. Satisfactory yields (up to 95%) were achieved using n-Bu2CuCNLi2 as the nucleophile and Et2O as the solvent. The reaction demonstrated successful incorporation of primary, secondary, tertiary and aromatic nucleophiles, as well as ring-openings of substrates bearing arene substituents and C1-bridgehead substituents. A generalized mechanism for these transformations is also proposed.