Synthesis of 3-Substituted Pyrrolidines via Palladium-Catalysed Hydroarylation

02 November 2018, Version 2
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

Metal-catalysed reactions have revolutionised synthetic chemistry, allowing access to unprecedented molecular architectures with powerful properties and activities. Nonetheless, some transformations remain sparse in number, or out of reach, even with the diverse modern catalytic chemical arsenal, including bimolecular alkene hydroarylation reactions. We report here the first palladium-catalysed alkene hydroarylation to give 3-aryl pyrrolidines, a class of small molecule with potency in a diverse range of biological scenarios. The process has broad substrate scope and can be used to directly deliver drug-like molecules in a single step from readily available precursors.

Keywords

Catalytic
Hydroarylation
Pyrrolidines
Dopaminergic
Serotonergic
HDAC inhibitors
Leishmaniasis

Supplementary materials

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Catalytic synthesis of 3-substituted pyrrolidines SI
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