Introduction
A domino process is a powerful tool to economically and sustainably build up complex molecular architectures which drastically reduces the number of work-up and purification steps. Recently, we developed new metal-free multi-step domino reactions and one-pot processes for the waste-reducing and cost-effective preparation of versatile frameworks, which otherwise are difficult to access via traditional methods. The developed new methods engage simple and readily available compounds in a wide range of domino reactions to construct e.g., azabicycles, quinazolines, quinazoline-thiohydantoins, 2,6-dicyanoanilines, o‐terphenyls and hexaarylbenzenes of interest for medicinal chemistry and materials science. Very recently, we disclosed a versatile autocatalytic transamination metathesis reaction, which is a multi-step domino process. This novel methodology gives rapid and atom-economical access to N-substituted 1,4-dihydropyridines, which are privileged structures in bioactive compounds and pharmaceuticals.
The in vitro tests against multidrug‐resistant P. falciparum strains (Dd2 and K1), human cytomegalovirus (HCMV), and multidrug-resistant P glycoprotein-overexpressing CEM/ADR5000 leukemia cells revealed the selected domino products and some corresponding artemisinin-containing hybrid compounds as highly active agents, outperforming the clinical reference drugs. These recent results will be discussed in the talk.
Selected references
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