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High Yielding, Multigram-Scale Synthesis of TBAJ-876 Fragment, 876A-B

24 April 2024, Version 2
Working Paper
This content is a preprint and has not undergone peer review at the time of posting.

Abstract

TBAJ-876 is an anti-tuberculosis drug shown to have high activity against multi-drug resistant tuberculosis (TB). We report a very efficient synthesis of the TBAJ-876 fragment 876A-B using an aldol condensation strategy starting from 6-bromo-3,4-dihydroquinolin-2(H)-one. The synthesis has been accomplished at multigram scale without the need of chromatography purification steps.

Keywords

tuberculosis
TBAJ
TBAJ-876
876A-B
bedaquiline
diarylquinoline

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Version History

Apr 24, 2024 Version 2

Version Notes

References section was left out of first version.

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The content is available under CC BY NC ND 4.0 [opens in a new tab]

DOI

10.26434/chemrxiv-2024-n6zr9-v2
D O I: 10.26434/chemrxiv-2024-n6zr9-v2 [opens in a new tab]

Funding

Bill and Melinda Gates Foundation

Author’s competing interest statement

The author(s) have declared they have no conflict of interest with regard to this content

Ethics

The author(s) have declared ethics committee/IRB approval is not relevant to this content

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