Ester as a blocking group for palladium-catalysed direct forced arylation at the unfavourable site of heteroaromatics: simple access to the less accessible regioisomers

Green Chemistry Pub Date: 2012-03-01 DOI: 10.1039/C2GC16460D

Abstract

The use of esters as blocking groups at the C2 position on a range of 3-substituted 5-membered ring heteroaromatics such as thiophenes or furans, allows control of the regioselectivity for the palladium-catalysed direct arylation at C5-H. This arylation can be followed by easy decarboxylation. This method allows sequential catalytic C5 arylation, decarboxylation and catalytic C2 arylation reactions.

Graphical abstract: Ester as a blocking group for palladium-catalysed direct forced arylation at the unfavourable site of heteroaromatics: simple access to the less accessible regioisomers
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