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A Rapid Total Synthesis of Ciprofloxacin Hydrochloride in Continuous Flow
Angewandte Chemie International Edition ( IF 16.6 ) Pub Date : 2017-06-20 , DOI: 10.1002/anie.201703812
Hongkun Lin 1 , Chunhui Dai 2 , Timothy F. Jamison 2 , Klavs F. Jensen 1
Affiliation  

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.

中文翻译:

连续流动快速快速合成盐酸环丙沙​​星

在9分钟的总停留时间内,环丙沙星的钠盐是由简单的结构单元通过在五个流动反应器中进行六个化学反应的线性序列而制备的。连续的离线酸化和过滤得到环丙沙星和盐酸环丙沙​​星。八步序列的总产率为60%。当进行单个酰化反应以去除主要副产物二甲胺时,在整个合成过程中无需分离中间体。
更新日期:2017-06-20
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