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A regioselective approach to the synthesis of benzo[h][1,6]‐naphthyridine and chromenopyrazinone derivatives was developed. The synthetic route to benzo[h][1,6]‐naphthyridines involves the N‐propargylation of aromatic aminobenzaldehydes, followed by reaction with propargylamine in the presence of DBU (1,8‐diazabicyclo[5.4.0]undec‐7‐ene). For the synthesis of chromenopyrazine and chromenopyrazinone...