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Enantioselective Synthesis of Fluoro–Dihydroquinazolones and −Benzooxazinones by Fluorination-Initiated Asymmetric Cyclization Reactions

Published Web Location

https://doi.org/10.1021/acscatal.5b02182
Abstract

Stereoselective synthesis of two fluorine-bearing drug-like scaffolds, dihydroquinazolone and benzooxazinone, has been accomplished through asymmetric fluorocyclization reactions initiated by the fluorination process. The reaction employs double axially chiral anionic phase-transfer catalysts to achieve high diastereo- and enantioselectivities, and a wide range of fluorine-containing dihydroquinazolones were obtained (>20:1 dr, up to 98% ee).

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