1,3-dipolar cycloaddition of azides and alkynes. I: Main synthetic aspects

Abstract

The concept of the "click" chemistry was introduced by Prof. Sharpless and coworkers in 2001 to define a modular synthetic approach that uses only the most practical and reliable chemical transformations. Among a number of reactions that meet these criteria, the Huisgen 1,3-dipolar cycloaddition of azides and alkynes, in particular the copper(I)-catalyzed version, has been established as the most effective and versatile. In the last years, its use has been spread exponentially in numerous applications within a variety of scientific fields including organic synthesis, molecular biology, and synthesis of new functional materials.