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Cu-Catalyzed Coupling Reactions of Sulfonamides with (Hetero)Aryl Chlorides/Bromides
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2022-09-06 , DOI: 10.1002/anie.202210483
Qiaoli Li 1 , Lanting Xu 2 , Dawei Ma 2
Affiliation  

Cu-catalyzed sulfonamidation of (hetero)aryl halides proceeds with excellent reaction scope by using oxalamides or 4-hydroxypicolinamides as the ligands. For bromides, only 2–5 mol % CuI and oxalamides were required. For chlorides, increasing catalytic loadings to 10 mol % Cu2O and ligands was needed. Direct sulfonamidation of four chloro-containing marketed drugs and preparation of two sulfonamide drugs were achieved under these conditions.

中文翻译:

磺胺类化合物与(杂)芳基氯/溴化物的铜催化偶联反应

通过使用草酰胺或 4-羟基吡啶甲酰胺作为配体,Cu 催化的(杂)芳基卤化物磺酰胺化反应具有出色的反应范围。对于溴化物,仅需要 2–5 mol% CuI 和草酰胺。对于氯化物,需要将催化负载增加到 10 mol% Cu 2 O 和配体。在此条件下实现了四种含氯市售药物的直接磺酰胺化和两种磺胺类药物的制备。
更新日期:2022-09-06
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