Background: The Hetero-Diels-Alder reaction (HDAR) is a method extensively used in organic
chemistry as a tool in the synthesis of innumerous polycyclic compounds in particular nitrogen compounds,
presents in many natural products, medicinally relevant substances and organic materials. The literature describes
innumerable studies of HDAR using classic methods and modern developments such as reactions on
the solid phase, the use of catalysts, transformations in aqueous solution and under microwaves.
Objective: This review describes a variety of HDAR focused on obtaining nitrogen-containing compounds of
considerable chemical and biological interest, and highlighting reported biological activity.
Conclusion: This review has shown the importance of the HDA reaction as a tool of organic chemistry in the
synthesis of nitrogen compounds. This type of reaction presents important properties including bond-forming
economy, high regio- and stereoselectivities and thus provides highly efficient routes to access a wide range of
polycyclic compounds. In addition to the variety of nitrogen compounds synthetized successfully by this
method, they present relevant biological properties.