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DMSO催化(杂)芳烃衍生物的氯化反应
Jiao的团队最近报道了在N-氯丁二酰亚胺(NCS)和催化量的DMSO的作用下(杂)芳烃的氯化反应。该反应以高收率和高区域选择性被应用于多种(杂)芳烃,例如吲哚,吡啶和噻吩等。此外,这种氯化方法还可以应用于萘普生和双氯芬酸等药物,盐酸罂粟碱和鬼臼毒素等天然产物,以及肽中酪氨酸残基的侧链。该氯化反应可以在中性、温和的条件下进行,因此有望用于药物研发的后期合成中。另外,与具有C-H键活化作用的铜介导的氯化反应相比,它具有易于操作和条件更温和的优势2,3)。
文献
- 1) DMSO-catalysed late-stage chlorination of (hetero)arenes
- 2) Regioselective copper-catalyzed chlorination and bromination of arenes with O2 as the oxidant
- 3) Para-Selective Halogenation of Nitrosoarenes with Copper(II) Halides