Synthesis of 4,5,6-trisubstituted-1,3-dihydroisobenzofurans by virtue of palladium-catalyzed domino carbopalladation of bromoenynes and internal alkynes

Abstract

An efficient hetero-annulation protocol has been developed for the construction of 4,5,6-trisubstituted-1,3-dihydroisobenzofurans via palladium-catalyzed domino carbopalladation of bromoenynes and internal alkynes. The reaction followed domino intramolecular Heck cyclization (5-exo-dig) and termination of the resulting diene with an internal alkyne to give highly substituted isobenzofurans in moderate to good yields.