聚乙二醇中咪唑与芳基硼酸的N-芳基化反应

N-Arylation Reaction of Imidazole with Arylboronic Acids in Poly( ethylene glycol)

N-芳基咪唑类化合物是一类非常重要的结构单元,常见于药物、农药以及生物分子中,因此寻找新的合成N-芳基咪唑类物质的方法成为有机合成化学家关注的热点问题之一。在绿色化学的倡导下,研究发展了一个促进咪唑类底物与芳基硼酸N-芳基化反应的催化体系,它是以Cu_2O(10%)为催化剂,以聚乙二醇400为反应介质,在室温下反应。研究结果表明,该催化体系适用于咪唑类底物与各种具有不同取代基的芳基硼酸的N-芳基化反应,为N-芳基咪唑类化合物提供一个简单、有效、绿色的合成方法。

N-Arylimidazole compounds are very important units which are commonly found in pharmaceuticals,medicines,and biological molecular. One of the hottest research topics in organic synthesis is to develop efficient and new catalytic systems for the synthesis of N-arylimidazole compounds. In this work,a new efficient and green catalytic system was developed for the N-arylation reaction of imidazole with arylboronic acids. Using Cu2O（ 10%） as a catalyst,poly（ ethylene glycol）-400（ PEG 400） as solvent,the N-arylation reaction of imidazole with arylboronic acids could proceed smoothly at room temperature,affording the desired Narylimidazole compounds in good yields.