Issue 21, 2016

Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions

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.

Graphical abstract: Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions

Supplementary files

Article information

Article type
Paper
Submitted
03 May 2016
Accepted
05 May 2016
First published
10 May 2016
This article is Open Access
Creative Commons BY-NC license

Org. Biomol. Chem., 2016,14, 4943-4946

Author version available

Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions

T. Flagstad, G. Min, K. Bonnet, R. Morgentin, D. Roche, M. H. Clausen and T. E. Nielsen, Org. Biomol. Chem., 2016, 14, 4943 DOI: 10.1039/C6OB00961A

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