Recent contributions to the Diversity-Oriented Synthesis (DOS) mediated by iminium ions through multicomponent Mannich-type reactions

Abstract

This short account summarizes the most recent contributions of the author and his collaborators to the Diversity Oriented Synthesis (DOS) mediated, at least in a step of the process, by Mannich-type reactions (MTR) and using formaldehyde as common starting material in all cases. Through this strategy, diverse nitrogen-containing acyclic and heterocyclic systems were synthesized, whether in straightforward or multicomponent approaches.

α-Halogenoacetamides: versatile and efficient tools for the synthesis of complex aza-heterocycles

“…The variety of structures reachable from these simple and tunable building blocks makes them good substrates for Diversity-Oriented Synthesis (DOS). [7][8][9][10] The amide function is probably the main group in biologically relevant compounds, and therefore, many efforts have been devoted to their formation. 11 α-Halogenoacetamides A (X = Cl, Br, I) play an important role 12 due to their ability to behave both as a nucleophile (at the nitrogen atom) and as an electrophile (at the carbon bearing the halogen) ( Figure 1).…”