Synthesis of 1-Borylisoindoles via Palladium-Catalyzed Dehydrogenation/C-H Borylation of Isoindolines

1-Boryl- and 1,3-diborylisoindoles were synthesized by the palladium-catatyzed reaction of isoindolines with pinacolborane via sequential dehydrogenation and C-H borylation. Selective formation of the borylated isoindoles was achieved using Pd(dba)(2)/Me2S as the catalyst, in which Me,S suppressed the formation of 1-boryl-4,5,6,7-tetrahydroisoindoles. Diborylisoindole was cross-coupled with iodobenzene, giving 1,3-diphenylisoindole in high yield.