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Metal‐Free, Oxidant‐Free, Site‐Selective C−H Halogenations to Aminoquinolines at Room Temperature using N ‐Halosaccharins
Author(s) -
Dutta Himangsu Sekhar,
Khan Bhuttu,
Khan Afsar Ali,
Ahmad Ashfaq,
Kant Ruchir,
Koley Dipankar
Publication year - 2017
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.201701649
Subject(s) - halogenation , regioselectivity , chemistry , organic chemistry , combinatorial chemistry , catalysis
We report a metal‐free, oxidant‐free, highly regioselective halogenations protocol (chlorination, bromination and iodination) to amidoquinolines using N ‐halosaccharin derivatives. Various amidoquinolines are tolerated by the method and delivered C5‐haloamidoquinoline derivates in excellent yields. A homo and hetero bis‐halogenation protocol has also been established. Late stage drug molecule diversification has also been demonstrated using the developed protocol.