Affiliation:
1. Institute of Chemistry Saint Petersburg State University Saint Petersburg 199034 Russian Federation
2. Saint Petersburg Research Institute of Phthisiopulmonology Saint Petersburg 191036 Russian Federation
Abstract
AbstractTetramic acids exhibit intriguing biological activity and are particularly attractive scaffolds for drug design. In this paper, we present a convenient approach based on the Dieckmann cyclization of Ugi adducts of malonic monoesters to afford a series of medically important polysubstituted tetramic acid derivatives. This simple and versatile method tolerates various substituents in both the amine, aldehyde and isocyanide moieties allowing the use of α‐substituted malonic acid monoesters. Examples of further functionalization of the free methylene group in the synthesized compounds have been presented.
Funder
Russian Science Foundation