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A chemoselective and continuous synthesis of m-sulfamoylbenzamide analogues

Authors
  • Verlee, Arno
  • Heugebaert, Thomas
  • van der Meer, Tom
  • Kerchev, Pavel
  • Van Breusegem, Frank
  • Stevens, Christian
Publication Date
Jan 01, 2017
Source
Ghent University Institutional Archive
Keywords
Language
English
License
Unknown
External links

Abstract

For the synthesis of m-sulfamoylbenzamide analogues, small molecules which are known for their bioactivity, a chemoselective procedure has been developed starting from m-(chlorosulfonyl) benzoyl chloride. Although a chemoselective process in batch was already reported, a continuous-flow process reveals an increased selectivity at higher temperatures and without catalysts. In total, 15 analogues were synthesized, using similar conditions, with yields ranging between 65 and 99%. This is the first automated and chemoselective synthesis of m- sulfamoylbenzamide analogues.

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