Chemistry - A European Journal p. 3832 - 3836 (2017)
Update date:2022-07-29
Topics:
Marelli, Enrico
Renault, Yohann
Sharma, Sunil V.
Nolan, Steven P.
Goss, Rebecca J. M.
The palladium-catalysed aqueous α-arylation of ketones was developed and tested for a large variety of reaction partners. These mild conditions enabled the coupling of aryl/alkyl-ketones with N-protected halotryptophans, heterocyclic haloarenes, and challenging base-sensitive compounds. The synthetic potential of this new methodology for the diversification of complex bioactive molecules was exemplified by derivatising prochlorperazine. The methodology is mild, aqueous and flexible, representing a means of functionalizing a wide range of halo-aromatics and therefore has the potential to be extended to complex molecule diversification.
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