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This paper describes a general method for the synthesis and the isolation of novel 2, or 3-halopyridin-4-yl-boronic acids and esters 12–14, 18–20. These compounds are prepared taking in account a regioselective halogen–metal exchange using nBuLi or directed ortho-metalation using LDA and subsequent quenching with triisopropylborate starting from appropriate mono or dihalopyridines. All substrates studied to date provided a single regioisomeric boronic acid or ester product. Additionally, these compounds have been found to undergo Pd-catalysed coupling with a range of arylhalides and authorise a strategy to produce new pyridines libraries. [Copyright &y& Elsevier]

This paper describes a general method for the synthesis and isolation of novel 6-halo-pyridin-3-yl-boronic acids and esters 2–5. These compounds are prepared taking in account a regioselective halogen–metal exchange with a trialkylborate starting from 2,5-dihalopyridines. All substrates studied to date provided a single regioisomeric boronic acid or ester product. Additionally, these compounds have been found to undergo Pd-catalysed coupling with a range of arylhalides and authorise a strategy to produce new pyridines libraries. [Copyright &y& Elsevier]