A Rapid Total Synthesis of Ciprofloxacin Hydrochloride in Continuous Flow

Hongkun Lin, Chunhui Dai, Timothy F. Jamison, Klavs F. Jensen

Angewandte Chemie International Edition · 2017 · 120 citations · 38 references

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Abstract

Within a total residence time of 9 min, the sodium salt of ciprofloxacin was prepared from simple building blocks via a linear sequence of six chemical reactions in five flow reactors. Sequential offline acidifications and filtrations afforded ciprofloxacin and ciprofloxacin hydrochloride. The overall yield of the eight-step sequence was 60 %. No separation of intermediates was required throughout the synthesis when a single acylation reaction was applied to remove the main byproduct, dimethylamine.

References

38