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Issue 21, 2016
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Synthesis of sp3-rich scaffolds for molecular libraries through complexity-generating cascade reactions

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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

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Publication details

The article was received on 03 May 2016, accepted on 05 May 2016 and first published on 10 May 2016


Article type: Paper
DOI: 10.1039/C6OB00961A
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Org. Biomol. Chem., 2016,14, 4943-4946
  • Open access: Creative Commons BY-NC license
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    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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