A metal-catalyzed enyne-cyclization step for the synthesis of bi- and tricyclic scaffolds amenable to molecular library production

Peng Wu; Michael Åxman Petersen; A. Emil Cohrt; Rico Petersen; Rémy Morgentin; Hugues Lemoine; Carine Roche; Anthony Willaume; Mads H. Clausen; Thomas E. Nielsen

doi:10.1039/C6OB01148A

A metal-catalyzed enyne-cyclization step for the synthesis of bi- and tricyclic scaffolds amenable to molecular library production†

Peng Wu,‡^a Michael Åxman Petersen,‡^a A. Emil Cohrt,‡^a Rico Petersen,^a Rémy Morgentin,^b Hugues Lemoine,^b Carine Roche,^b Anthony Willaume,^b Mads H. Clausen*^ac and Thomas E. Nielsen*^ad

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^a Department of Chemistry, Technical University of Denmark, Kgs. Lyngby, Denmark
E-mail: ten@sund.ku.dk

^b EDELRIS, 115 Avenue Lacassagne, 69003 Lyon, France

^c Center for Nanomedicine and Theranostics, Technical University of Denmark, Kgs. Lyngby, Denmark

^d Singapore Centre on Environmental Life Science Engineering, Nanyang Technological University, Singapore

Abstract

A facile metal-catalyzed diversification step for the synthesis of novel bi- and tricyclic scaffolds from enyne substrates is reported in this study. From a single starting material, topologically diverse scaffolds for library synthesis can be generated and decorated in a few steps. The methodology was used to produce a library of 490 compounds within the European Lead Factory (ELF) Consortium.

This article is part of the themed collection: Contemporary Synthetic Chemistry in Drug Discovery

Organic & Biomolecular Chemistry

A metal-catalyzed enyne-cyclization step for the synthesis of bi- and tricyclic scaffolds amenable to molecular library production†

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A metal-catalyzed enyne-cyclization step for the synthesis of bi- and tricyclic scaffolds amenable to molecular library production

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