Mild, Aqueous α-Arylation of Ketones: Towards New Diversification Tools for Halogenated Metabolites and Drug Molecules.
Chemistry
; 23(16): 3832-3836, 2017 Mar 17.
Article
em En
| MEDLINE
| ID: mdl-28195381
ABSTRACT
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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MEDLINE
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Paládio
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Hidrocarbonetos Aromáticos
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Cetonas
Idioma:
En
Ano de publicação:
2017
Tipo de documento:
Article