Synthetic Approaches Towards the Synthesis of C-1 Azole Substituted Tetrahydroisoquinolines

Abstract

C-1 substituted tetrahydroisoquinolines have emerged as important scaffolds in pharmaceutical and medical research. Although various methods for α-substitution on tetrahydroisoquinolines have been discovered, the introduction of the azole group at C-1 position remains a challenge. Recently, direct C-H activation methods and multicomponent reactions have been employed towards the synthesis of azole containing tetrahydroisoquinolines. A summary of such synthetic strategies is presented here as these promising methods can help in developing more efficient synthetic routes. This minireview covers the available synthetic methods and their mechanistic pathways for the preparation of C-1 azole substituted tetrahydroisoquinolines.