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

24 April 2024, Version 2
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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