无催化剂合成芳基磺酰基吲哚的三组分反应

Catalyst-free Synthesis of 3-( 1-arylsulfonylalkyl) indoles via Three-component Reaction

Friedel-Crafts烷基化反应是有机化学中最重要的C-C键形成反应之一。这些反应通常由质子酸或路易斯酸催化辅助。吲哚及其许多衍生物存在于自然界中常见的多种化合物,以及具有比较好的药理和生物学活性的化合物。在室温下吲哚、苯甲醛和芳烃的无催化剂三组分反应提供了直接合成重要的3-(1-芳基磺酰基)吲哚的途径。该反应条件温和,操作简单成本低,底物范围广,原子利用率高。

Friedel-crafts alkylation is one of the most important C-C bond-forming reactions in organic chemistry.These reactions are usually assisted by either protic acid or Lewis acid catalyst.Indoles and many of its derivatives are present in numerous substances commonly found in nature,as well as in the compounds that show pharmacological and biological activities.A catalyst-free three-component reaction of indoles,carbonyls and arenesulfinic acids performed at room temperature provides direct access to biologically important 3-(1-arylsulfonylalkyl)indoles.This process features mild conditions,low cost,broad substrate scope and high yields.