A chemoselective and continuous synthesis of <i>m</i>-sulfamoylbenzamide analogues
作者:Arno Verlee、Thomas Heugebaert、Tom van der Meer、Pavel I Kerchev、Frank Van Breusegem、Christian V Stevens
DOI:10.3762/bjoc.13.33
日期:——
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
为了合成以其生物活性而闻名的小分子氨磺酰基苯甲酰胺类似物,已从间氯磺酰基苯甲酰氯开始开发了一种化学选择性方法。尽管已经报道了分批进行化学选择的方法,但是连续流方法显示出在较高温度下且没有催化剂的情况下选择性的提高。在相似的条件下,总共合成了15种类似物,产率在65%至99%之间。这是间氨基磺酰基苯甲酰胺类似物的首次自动化和化学选择性合成。