Palladium-Catalyzed Strain-Enabled [2π + 2σ] Cycloadditions of Vinyl Bicyclo[1.1.0]butanes with Methyleneindolinones

Org Lett. 2024 Dec 26. doi: 10.1021/acs.orglett.4c04224. Online ahead of print.

Abstract

A palladium-catalyzed [2π + 2σ] cycloaddition of vinyl bicyclo[1.1.0]butanes with methyleneindolinones has been developed. The reaction enables the construction of spirobicyclo[2.1.1]hexanes bearing an all-carbon quaternary center in moderate to good yields with excellent diastereoselectivities. This method features a broad substrate scope with good functional group compatibility. The practical utility of this protocol was further demonstrated by gram-scale synthesis and postsynthetic transformations of desired product.