Issue 15, 2022

Practical synthesis of quinolone drugs via a novel TsCl-mediated domino reaction sequence

Abstract

A novel TsCl-mediated domino sequence to expeditiously access quinolone-based antibiotics, such as ciprofloxacin, norfloxacin, pefloxacin, oxilinic acid, ivacaftor and the precursor of grepftfloxacin and ozenoxacin, starting from commercially available chromone-3-carboxaldehydes and amines, was developed. The total synthesis of these quinolone-based drugs via this sequence shortens the original seven/eight step synthesis to three/four steps with a high overall yield under environmentally benign conditions. The quinolone-based antibiotic drug analogues could also be efficiently synthesized by varying the starting materials and chemical reagents for discovering and developing new antibiotics.

Graphical abstract: Practical synthesis of quinolone drugs via a novel TsCl-mediated domino reaction sequence

Supplementary files

Article information

Article type
Communication
Submitted
06 5月 2022
Accepted
15 6月 2022
First published
08 7月 2022

Green Chem., 2022,24, 5755-5759

Practical synthesis of quinolone drugs via a novel TsCl-mediated domino reaction sequence

J. Lei, Y. Ding, H. Zhou, X. Gao, Y. Cao, D. Tang, H. Li, Z. Xu and Z. Chen, Green Chem., 2022, 24, 5755 DOI: 10.1039/D2GC01689C

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