We thank the Oregon Health & Science University Medicinal Chemistry Core Department (Portland, OR) for the use the Biotage® Initiator+ microwave synthesizer. This project was supported by NIH/NIAID (award 1R01AI093784) and DOD/PRMRP (award PR160693/W81XWH-17-2-0041).
Malaria -- Prevention -- Research
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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Kancharla, P., Dodean, R. A., Li, Y., & Kelly, J. X. (2019). Boron trifluoride etherate promoted microwave-assisted synthesis of antimalarial acridones. RSC Advances, 9(72), 42284-42293.