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Published on: June 23, 2019
Boron Trifluoride Etherate Promoted Microwave-Assisted Synthesis of Antimalarial Acridones
Papireddy Kancharla1, Rozalia A Dodean1,2, Yuexin Li1,2
1Department of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Abstract:
A microwave-assisted, rapid and efficient method using boron trifluoride etherate (BF3.Et2O) 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.
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