Accessing Tri-substituted γ-Lactam Scaffolds Via Cascade Reactions: What Opportunities For Libraries!

Karine Bonnet, Mads Hartvig Clausen, Nicolas Fleury-Brégeot, Claude Lardy, Rémy Morgentin, Thomas Eiland Nielsen, Michael Åxman Petersen, Martin Ohsten Rasmussen, Didier Roche, Peng Wu

Research output: Contribution to journalConference abstract in journalResearchpeer-review

Abstract

The European Lead Factory is an EU-based initiative (part of the Innovative Medicines Initiative), which has been set to foster drug discovery in Europe. Among the objectives, a 200,000-compound collection is being generated.Lactams represent a large class of valuable scaffolds for medicinal chemistry and remain a wide and interesting area of study. In this context, 2 libraries based on a 1,4,5 γ-lactam core have been designed and produced using cascade reactions involving an aldehyde moiety, an amine and a nucleophilic partner as the key reaction. One library is focused on a 3-MCR on oxo-esters, while the other is based on a Ritter-type cascade. On several occasions these multi-component and one-pot processes have been used directly as the production step, thus allowing very fast and diverse library syntheses, whereas in other cases, the choice of partners bearing other anchoring groups permitted further functionalization and the production of even more diverse members of the libraries. The > 1,000 compounds based on these scaffolds have been delivered for HTS at the European Screening Center where they are currently being tested.
Original languageEnglish
JournalF A S E B Journal
Volume30
Issue number1
ISSN0892-6638
Publication statusPublished - 2017
EventExperimental Biology 2016 Meeting: Transforming the future through science - San Diego, United States
Duration: 2 Apr 20166 Apr 2016
http://experimentalbiology.org/2016/home.aspx

Conference

ConferenceExperimental Biology 2016 Meeting
CountryUnited States
CitySan Diego
Period02/04/201606/04/2016
Internet address

Cite this

Bonnet, K., Clausen, M. H., Fleury-Brégeot, N., Lardy, C., Morgentin, R., Nielsen, T. E., Petersen, M. Å., Rasmussen, M. O., Roche, D., & Wu, P. (2017). Accessing Tri-substituted γ-Lactam Scaffolds Via Cascade Reactions: What Opportunities For Libraries! F A S E B Journal, 30(1).