Synthesis of [6,5,5]Ring-Fused Tricyclic Triazoles by Copper-Promoted Double Cyclization

Abstract

Ring-fused 1,2,3-triazoles are important biologically active compounds and synthetic intermediates. Known methods for their synthesis are limited mostly to triazoles fused to six-membered or larger rings. Herein we disclose a synthetic approach to triazoles fused to five-membered rings based on copper(I)-promoted double cyclization consisting of azide-alkyne cycloaddition, followed by cross coupling to aryl iodides.