Glycosyl Radical-Based Synthesis of C-Alkyl Glycosides Bearing a Cyclopropane via a Deoxygenative Giese Addition-Reduction-Cyclization Cascade

Org Lett. 2025 Jan 10;27(1):504-509. doi: 10.1021/acs.orglett.4c04510. Epub 2024 Dec 23.

Abstract

We have developed a glycosyl radical-based synthesis of C-alkyl glycosides through a deoxygenative Giese addition-reduction-cyclization cascade, in which readily available 1-hydroxy carbohydrates serve as precursors for glycosyl radicals and aryl alkenes function as radical acceptors. This reaction not only provides an effective method for accessing a previously underexplored class of functionalized cyclopropanes but also enhances the application of Giese addition in the synthesis of C-alkyl glycosides by derivatizing the radical intermediate generated through polar cyclization to yield a cyclopropane.