European Journal of Organic Chemistry p. 2339 - 2343 (2019)
Update date:2022-09-26
Topics:
Heeran, Darren
Sandford, Graham
Sequential reaction cascades for the synthesis of polysubstituted 2- and 3-fluoropyrrole derivatives from common polybromopyrrole precursors have been developed. A strategic variation of a combination of regioselective debromolithiation followed by trapping of the corresponding carbanions by electrophilic fluorination and Pd catalysed cross-coupling reactions allows access to polyfunctional fluoropyrrole products by methodology applicable to drug discovery programs, extending the range of five-membered fluoroazaheteroaromatic derivatives potentially available for incorporation into screening libraries.
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