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Application of Continuous Flow in Tazobactam Synthesis
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-06-17 , DOI: 10.1021/acs.oprd.1c00127
Shuhao Zhou 1 , Yunting Xin 1 , Jiasheng Wang 1 , Chengjun Wu 1 , Tiemin Sun 1
Affiliation  

Tazobactam is a β-lactamase inhibitor. In this work, a combination of continuous flow and batch experiments for the synthesis of tazobactam has been developed. The first three steps and the preparation of the peroxyacetic acid are continuously carried out in the microreactors, which improves the procedure safety and efficiency. There is also a final step of the deprotection reaction in the microreactor, which can increase the yield and reduce the formation of impurities. Under optimized process conditions, the total yield of the target product reached 37.09% (30.93% in batch). The continuous flow method not only greatly reduces the reaction time but also significantly improves procedure safety and increases the yield.

中文翻译:

连续流在他唑巴坦合成中的应用

他唑巴坦是一种β-内酰胺酶抑制剂。在这项工作中,已经开发了用于合成他唑巴坦的连续流动和间歇实验的组合。前三步和过氧乙酸的制备在微反应器中连续进行,提高了程序的安全性和效率。微反应器中还有脱保护反应的最后一步,可以提高收率,减少杂质的形成。在优化的工艺条件下,目标产品的总收率达到37.09%(批量为30.93%)。连续流法不仅大大缩短了反应时间,而且显着提高了程序的安全性,提高了收率。
更新日期:2021-07-16
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