'Click’ Chemistry,直译为“点击化学”。在2001年,Sharpless在Angew上发表了题为《Click Chemistry: Diverse Chemical Function from a Few Good Reactions》的综述,系统阐释了点击化学的定义与应用。
事实上,点击化学最早描述为“ Following nature's lead, we endeavor to generate substances by joining small units together with heteroatom links (C-X-C). The goal is to develop an expanding set of powerful, selective, and modular blocks that work reliably in both small- and large-scale applications. ”即通过杂原子连接将两个分子砌块结合起来,从而得到多样化、普适的分子库。 点击化学的特点是:模块化(modular),多样化(wide in scope),高产率(give very high yields),只产生非柱色谱可分离的副产物(generate only inoffensive byproducts that can be removed by nonchromatographic methods),立体专一 (stereospecific)。 最广为人知的点击化学的反应是叠氮和炔的1,3-偶极环加成,得到一个1,2,3-三唑。