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

Jie Lei, Yong Ding, Hao Yi Zhou, Xin Yan Gao, Yi Hua Cao, Dian Yong Tang, Hong Yu Li, Zhi Gang Xu, Zhong Zhu Chen

Research output: Contribution to journalArticlepeer-review

4 Scopus citations

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.

Original languageEnglish (US)
Pages (from-to)5755-5759
Number of pages5
JournalGreen Chemistry
Volume24
Issue number15
DOIs
StatePublished - Jul 8 2022
Externally publishedYes

ASJC Scopus subject areas

  • Environmental Chemistry
  • Pollution

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