One-pot simultaneous debrominative decarboxylation and sulfamation of anti-2,3-dibromo-3-(4- chlorosulfonylphenyl)propanoic acid in DMF (for alkylamines) or DMF-pyridine (1/1, for arylamines) using a diverse range of alkyl and aryl amines under microwave irradiation stereoselectively afforded intermediate (Z)-4-(2-bromovinyl)benzenesulfonamides. The intermediates, without isolation and purification, were treated with EtONa to give the desired 4-ethynylbenzenesulfonamides.
在
DMF(对于烷基胺)或
DMF-
吡啶(1/1,对于芳基胺)中,使用多种烷基和芳基胺在微波辐射下同时进行反
溴脱羧和磺化反应,立体选择性地得到中间体(Z)-4-(2-
溴乙烯基)苯磺酰胺。中间体未经分离和纯化,经EtONa处理后得到所需的4-
乙炔基苯磺酰胺。