A Unified Synthesis of Bifunctional 4‐Substituted‐1,2,3,4‐tetrahydroisoquinoline Derivatives

Abstract Starting from a single, commercially available bromoisoquinoline, convenient (multigram) syntheses of 4‐substituted‐1,2,3,4‐tetrahydroisoquinoline derivatives have been developed. The compounds thus prepared show suitable substitution patterns for further derivatization and constitute a new family of compounds of potential pharmacological interest. Keywords: Nucleophilic aromatic substitutionsProtecting groupsCombinatorial chemistryCopperHydrogenation Acknowledgments Financial support from the DGICYT, Spain (project BQU2000‐0235) is gratefully acknowledged. Drs Dolors Fernández and Juan Miguel Jiménez (Almirall Prodesfarma, Barcelona) are thanked for useful suggestions.