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A new synthetic method, which achieves regiospecific functionalization of 8-methylquinoline derivatives at C-2 and subsequent selective hydrogenation of the pyridine ring in a one-pot tandem process, has been reported. With this method, a total of thirteen new 8-methyltetrahydroquinoline derivatives with an amide side chain at C-2 were synthesized in moderate yields. The scope of substrates was investigated, and the reaction mechanism was studied and proposed.

Synthesis of 8-Methyltetrahydroquinoline derivatives functionalized at C-2: a one-pot tandem approach