Modular Click Chemistry Libraries for Functional Screens Using a Diazotizing Reagent

Barry Sharpless and Jiajia Dong present the use of a diazotizing reagent for modular click chemistry libraries.

Click chemistry – a term coined by 2001 Chemistry Nobel Prize Laureate Professor Barry Sharpless, at Scripps Research (USA) – aims to be a quick and modular synthesis concept for finding new molecules with desirable properties. Professor Sharpless had the intention of connecting two or three modules together in solution, in sequence, within a few hours and submitting the mixture directly to screening. With the discovery of the CuAAC triazole annulation reaction in 2002 nearly all of the group’s needs for intermolecular ligation were solved. According to Professor Jiajia Dong from the Sharpless laboratory, “it has been known for years that the CuAAC reaction is unusually predictable; however, it relies on the power of two highly energetic functional groups nature did not use, which kills the accessibility aspect. The commercial availability of both groups is very low compared to those that medicinal chemists often use.” The exciting discovery of the described methodology has an interesting origin, partially based on serendipity. In fact, during their experiments, the group wanted to use FSO2N3 for the SuFEx reaction and accidentally discovered the abnormal diazo-transfer process.

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