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Transition-metal-free site-selective C–F bond activation for synthesis of 8-aminoquinolines

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Abstract An efficient and general selective method for the synthesis of 8-aminoquinoline derivatives has been disclosed through transition metal direct C–N coupling from fluoroquinolines and arylamines. Significantly, good chemo- and… Click to show full abstract

Abstract An efficient and general selective method for the synthesis of 8-aminoquinoline derivatives has been disclosed through transition metal direct C–N coupling from fluoroquinolines and arylamines. Significantly, good chemo- and regio-selectivity was observed for polyfluoroquinolines in which only C–F bond on 8-substituted position was broken. Thus, this methodology proves its value as an inexpensive and efficient synthetic way to access quinolin-8amine derivatives in moderate to good yields.

Keywords: transition metal; site selective; bond; free site; metal free; synthesis

Journal Title: Tetrahedron Letters
Year Published: 2017

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