Silver triflate and triflic anhydride-promoted expedient synthesis of acylated 1-aminoisoquinolines

摘要

A practical and convergent synthesis of biologically active 1-(N-acyl)-1-aminoisoquinolines from the reaction of 2-alkynylbenz-aldoximes with amides has been realized. The readily available amides could be activated with triflic anhydride (Tf_2O) and could efficiently participate in the domino reaction of 2-alkynylbenz-aldoximes when catalyzed by AgOTf, thus providing various acylated 1-aminoisoquinolines with up to 98% yields.