Synthesis of CF3-Containing 1,2,3,4-Tetrahydroisoquinoline-3-Phosphonates via Regioselective Ruthenium-Catalyzed Co-cyclotrimerization of 1,7-Azadiynes.

An efficient access to novel trifluoromethyl-substituted phosphonate analogues of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (TIC) derivatives based on regioselective rutheniumcatalyzed co-cyclotrimerization of functionalized 1,7-diynes with various alkynes has been developed using RuClCp"cod and preferably Grubbs second-generation catalysts. [ABSTRACT FROM AUTHOR]