DOI: 10.1055/a-2899-9281 ISSN: 0039-7881

Decarboxylative Recyclization of 3-Isocyanatoisochroman-1-ones

Roman Y. Vasylyshyn, Bohdan A. Demydchuk, Vasyl S. Matiychuk, Oleg Lukin, Grygoriy A. Dolgonos, Svetlana Shishkina, Alexander Shivanyuk, Yevhen Karpun, Sergiy M. Kovalenko, Volodymyr Fetyukhin

A previously unknown decarboxylative recyclization of 3-isocyanato-isochroman-1-ones occurs at 200-220°C in PhOPh solution to afford a series of pharmacophoric isoquinolin-1(2H)-ones in 89-94% yield on a 4-8 gram scale. DFT-D calculations predict the exothermicity and entropic favorability of the rearrangement and suggest it’s possible mechanism

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