A chemoselective and continuous synthesis of m-sulfamoylbenzamide analogues

• Arno Verlee,
• Thomas Heugebaert,
• Tom van der Meer,
• Pavel I. Kerchev,
• Frank Van Breusegem and
• Christian V. Stevens

Beilstein J. Org. Chem. 2017, 13, 303–312, doi:10.3762/bjoc.13.33

• Systems Biology, VIB, Ghent University, Technologiepark 927, B-9000 Ghent, Belgium Department of Plant Biotechnology and Bioinformatics, Ghent University, Technologiepark 927, B-9052 Ghent, Belgium 10.3762/bjoc.13.33 Abstract For the synthesis of m-sulfamoylbenzamide analogues, small molecules which are

• , 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. Keywords: flow chemistry; medium-throughput synthesis; m-sulfamoylbenzamide analogues; Introduction Small

• be effective against Huntington’s and Parkinson’s disease [12][13][14]. They inhibit the Sirtuin 2 (SIRT2) deacetlyse protein (Figure 1, AK-1, AK-7) resulting in improved motor skills [12][13][15]. Furthermore, m-sulfamoylbenzamide analogues (Figure 1, C2-8) are able to suppress polyglutamine (polyQ