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Boron trifluoride etherate promoted microwave-assisted synthesis of antimalarial acridones

A microwave-assisted, rapid and efficient method using boron trifluoride etherate (BF(3).Et(2)O) for the synthesis of acridones, via an intramolecular acylation of N-phenylanthranilic acid derivatives, has been developed. The reaction proceeds under solvent-free conditions, tolerates a wide range of...

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Detalles Bibliográficos
Autores principales: Kancharla, Papireddy, Dodean, Rozalia A., Li, Yuexin, Kelly, Jane X.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8939876/
https://www.ncbi.nlm.nih.gov/pubmed/35321096
http://dx.doi.org/10.1039/c9ra09478d
Descripción
Sumario:A microwave-assisted, rapid and efficient method using boron trifluoride etherate (BF(3).Et(2)O) for the synthesis of acridones, via an intramolecular acylation of N-phenylanthranilic acid derivatives, has been developed. The reaction proceeds under solvent-free conditions, tolerates a wide range of functional groups, and provides rapid access to a range of acridones in good to excellent yields. Several of the synthesized acridones exhibited potent antimalarial activities against CQ sensitive and multi-drug resistant (MDR) parasites.