Abstract

Herein, we report the first atroposelective C(sp2)–H bond acyloxylation enabled by a phosphine oxide directing group. Uniquely, this transformation is shown to proceed through an eight-membered palladacycle intermediate, as opposed to the kinetically and thermodynamically favored five-membered palladacycle intermediate. Additionally, l-pGlu-OH, a cheap and abundant chiral amino acid derivative, was identified as the best chiral ligand to promote this atroposelective remote CH functionalization reaction.

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