Copper(I) iodide efficiently catalyzes deformylative C-N coupling of formamides and isoindolinone3-ols to provide C(3) primary/secondary amine substituted isoindolinones. The transformation requires a stoichiometric amount of phenylboronic acid as a co-reactant. In the reaction, formamides act as the synthetic equivalent of primary/secondary amines. The method is amenable for the synthesis of a combinatorial library of medicinally relevant C(3) amino substituted isoindolinones.
