The cyclization of amino-alkynes 1 in which an amino group is attached to the aromatic ring, proceeded smoothly using a catalytic amount of Pd (PPh3) 4 and benzoic acid in toluene at 120° C, leading to the formation of the 2-substituted tetrahydroquinolines 2. An asymmetric variant of the reaction using the chiral palladium catalyst (prepared in situ by mixing Pd2 (dba) 3⊙ CHCl3 and (R, R)-RENORPHOS) was also explored. The absolute ...
