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The first synthesis of 3-methoxalylchromone was described. The reaction of the latter with electron-rich aminoheterocycles afforded a set of heteroannelated pyridines bearing a CO2Me substituent located at the α-position of the pyridine core.

Graphical abstract: 3-Methoxalylchromone—a novel versatile reagent for the regioselective purine isostere synthesis

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