Matthias D’Hooghe
Ghent University, Belgium
Title: Application of small-ring azaheterocyclic building blocks for the synthesis of pharmaceutically relevant nitrogen compounds
Biography
Biography: Matthias D’Hooghe
Abstract
Small-ring azaheterocyclic systems have acquired a pivotal position as building blocks in medicinal chemistry. In particular, aziridines, azetidines and beta-lactams have been shown to be eligible synthons for the construction of a broad variety of stereodefined heterocyclic frameworks, often endowed with pronounced biological activities. In this presentation, the synthetic flexibility of these three- and four-membered systems toward the preparation of different types of pharmaceutically relevant nitrogen-containing target structures will be explained. In that respect, a number of novel synthetic strategies toward a broad set of important heterocyclic scaffolds will be discussed (see figure below). In particular, different new methods for the regio- and stereoselective rearrangement of aziridines, azetidines and beta-lactams into functionalized four- to seven-membered hetero (bi)cycles will be disclosed. All these compounds represent relevant moieties encountered as substructures in a variety of biologically active natural products and pharmaceuticals.