Boron Trifluoride Etherate Promoted Microwave Assisted Synthesis of Antimalarial Acridones

Authors

Papireddy Kancharla, Portland State UniversityFollow
Rozalia A. Dodean, Portland State UniversityFollow
Yuexin Li, Portland State UniversityFollow
Jane X. Kelly, Portland State UniversityFollow

Sponsor

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).

Published In

RSC Advances

Document Type

Article

Publication Date

2020

Subjects

Malaria -- Prevention -- Research

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.

Description

Open Access Article This Open Access Article is licensed under a Creative Commons Attribution-Non Commercial 3.0 Unported Licence

Locate the Document

10.1039/C9RA09478D

DOI

10.1039/C9RA09478D

Persistent Identifier

https://archives.pdx.edu/ds/psu/32680

Citation Details

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.