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Tetrahedron 2014, 70, 2370. DOI: 10.1016/j.tet.2014.02.040 ◆ Research group at Takeda found a practical synthetic method for 3-formylquinoline 12 using a stable vinamidinium salt to react with aniline derivative 11. ◆ The method using the triformylmethane synthon involves three chemical transformations: Schiff base formation with the aniline moiety, cyclization at the ortho position of aniline, and introduction of the formyl group at the 3-position of the quinoline. ◆ By newly developing the 2-iminomethylvinamidinium trihalides as stable salts with nondeliquescent nature in air, the research group achieved a scaled-up synthesis of 24.3 kg of quinoline 12.
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