EFFECT OF THE USE OF BULKY ALKYLPHOSPHINES IN THE SONOGASHIRA COUPLING WITH AQUEOUS AMMONIA

摘要

The Sonogashira coupling of terminal alkynes and aryl bromides with aqueous ammonia catalyzed by the in situ formed palladium complex of a bulky alkylphosphine furnishes the coupling product at room temperature. One-pot reaction of the Sonogashira coupling and the following intramolecular cyclization with 2-hydroxy or 2-amino aryl bromide leads to a facile synthesis of benzofuran and indole derivatives.