微波促进的点击化学

Microwave-Assisted Click Chemistry

自2001年Sharpless等提出点击化学概念以来,Cu(I)催化的炔与叠氮之间的1,3-偶极环加成反应(Cue-AAC)已经成为点击化学最成功的范例.Cue-AAC反应由于其良好的立体选择性、模块性以及官能团耐受性等特点迅速成为许多研究领域,例如药物化学、材料科学等领域中的有力工具.同时,微波加热作为一种高效、绿色合成技术已越来越受到人们的重视,相对于传统加热方式,它能大幅缩短反应时间,提高产率和纯度.综述了近十年来利用微波加热与点击化学相结合的策略在合成生物大分子及小分子化合物库中的应用,并对其发展前景作了展望.

Cu（I）-catalyzed azide-alkyne 1,3-dipolar cycloaddition（Cue-AAC）,which is the best paradigm of ＂Click Chemistry＂ philosophy that was initially coined by Sharpless and co-workers at the very beginning of the third millennium,has been demonstrated as a powerful tool in numerous scientific fields including medicinal chemistry,materials science,etc.,due to its superior stereoselectivity,modularity and functional group tolerance.Meanwhile,microwave irradiation has attracted increasingly much attention as a highly effective and green synthetic complement as this technique can distinctly reduce the time consumption and simultaneously enhance the yields and purity of a diverse range of organic reactions in comparison with conventional heating methods.Herein,recent tactics that combine Cue-AAC with microwave irradiation technique toward the construction of useful bio-macromolecules and small molecule libraries are reviewed while the prospective with respect to the future development of this specific area is offered.