Lei, Chuan-HuWang, De-XianZhao, LiangZhu, JiepingWang, Mei-Xiang2013-04-092013-04-092013-04-09201310.1021/ja401701xhttps://infoscience.epfl.ch/handle/20.500.14299/91397WOS:000317032000034A novel strategy for de novo synthesis of pyridines featuring an unprecedented a-addition of aldehyde and enamide to isonitrile as a key step is described. Under mild conditions, a cascade reaction involving Zn(OTf)(2)-promoted [1 + 5] cycloaddition of isonitrile with N-formylmethyl-substituted enamide, facile aerobic oxidative aromatization and intermolecular acyl transfer from the pyridinium nitrogen to the 5-hydroxy oxygen, and finally acylation of the 4-amino group by an external acyl chloride efficiently afforded 2-substituted 4-acylamino-5-acyloxypyridines in good to excellent yields.text::journal::journal article::research article