Copper (cat) and phenylboronic acid mediated deformylative C-N coupling of isoindolinone-3-ols with formamides provide C(3) aminoisoindolinones

Copper(I) iodide efficiently catalyzes deformylative C-N coupling of formamides and isoindolinone-3-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. Graphical Abstract Copper(I) iodide efficiently catalyzes deformylative C-N coupling of formamides and isoindolinone-3-ols in presence of stoichiometric amount of phenylboronic acid (co-reactant) to provide C(3) primary/secondary amine substituted isoindolinones. Here, formamides act as synthetic equivalents of primary/secondary amines. Herein we report synthesis of a combinatorial library of medicinally relevant C(3) amino substituted isoindolinones.