Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions. Issue 21 (12th May 2016)

• Record Type: Journal Article
• Authors: Flagstad, T.; Min, G.; Bonnet, K.; Morgentin, R.; Roche, D.; Clausen, M. H.; Nielsen, T. E.
• Is Part Of: Organic & biomolecular chemistry. Volume 14:Issue 21(2016)
• Page Start: 4943
• Page End: 4946
• Publication Date: 2016-05-12
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c6ob00961a
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : An efficient strategy for the synthesis of complex small molecules from simple building blocks is presented. Abstract : An efficient strategy for the synthesis of complex small molecules from simple building blocks is presented. Key steps of the strategy include tandem Petasis and Diels–Alder reactions, and divergent complexity-generating cyclization cascades from a key dialdehyde intermediate. The methodology is validated through the synthesis of a representative compound set, which has been used in the production of 1617 molecules for the European Lead Factory.