A tris(pentafluorophenyl)borane catalysed method for the synthesis of boronic acid esters from aromatic amines in yields of up to 93% was devised. Mild conditions, benign reagents, short reaction times, low temperatures and a wide substrate scope characterize the method. The reaction was found applicable to the synthesis of boronic acid ester derivatives of complex drug molecules in up to 86% isolated yield and high purity suitable for labelling. These boronates were subsequently labelled with [F]fluoride ion in radiochemical yields of up to 55% with and even without isolation of the boronate-intermediate.
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| http://dx.doi.org/10.3389/fchem.2022.884478 | DOI Listing |
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