Direct Functionalization of Benzoquinolines

The first direct lithiation of the pyridine ring of benzo[h]- and benzo[f]- quinolines is reported. The method allowed the introduction of different electrophiles (Cl, Br and SPh) in 2-position. Other groups were introduced by direct nucleophilic addition of alkyllithiums allowing further transformations to functional groups such as esters and thiolesters.