Facile, solvent and ligand free iron catalyzed direct functionalization of N-protected tetrahydroisoquinolines and isochroman

摘要

An efficient method for an iron catalyzed oxidative indolation and methoxyphenylation of N-protected tetrahydroisoquinolines and isochroman is described including subsequent facile deprotection. Tetrahydroisoquinolines (THIQs) and indoles are common substructures in natural products and Pharmaceuticals.Moreover, 1-aryl tetrahydroisoquinoline analogues are potential neuroprotective agents and act as anti-HIV agents in vitro. Methods for the efficient preparation of such compounds are therefore highly welcome.