Hydroxyl-directed C-H carbonylation enabled by mono-N-protected amino acid ligands: An expedient route to 1-isochromanones

A Pd(II)-catalyzed C-H carbonylation protocol of phenethyl alcohols has been developed using amino acid ligands to promote the reaction. This transformation provides an expedient route to 1-isochromanone motifs, which are common structural elements in natural products and other biologically active compounds. A concise synthesis of a histamine release inhibitor showcases the utility of this transformation.