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奥美普林的合成工艺改进
Improvement of Synthesis Process of Ormetoprim
【摘要】 5-(4,5-二甲氧基-2-甲基苄基)-2,4-二氨嘧啶,又称为奥美普林,是一种抗菌增效剂,常与磺胺类抗菌药合用,可扩大磺胺类抗菌药的抗菌谱,显著提高磺胺类抗菌药的抗菌效果。在前人研究的基础上对奥美普林的合成工艺进行了改进,采用溴素代替原工艺中氢溴酸的卤代反应,避免了氧气的制备与应用,条件更加温和,增加了整个工艺中的可操作性,更适用于工业化大生产。此外还对工艺中工艺条件进行了筛选,确定了最佳的反应条件。
【Abstract】 5-(4,5-dimethoxy-2-methylbenzyl)-2,4-diaminopyrimidine, also known as ormetoprim, is an antibacterial synergist, which is often used with sulfonamides to expand the antibacterial spectrum of sulfonamides and significantly improve the antibacterial effect of sulfonamides. The synthesis process of omeprin was improved on the basis of previous studies. Bromine was used to replace the halogenation reaction of hydrobromic acid in the original process, which avoided the preparation and application of oxygen, and the conditions were milder, which increased the operability of the whole process and was more suitable for industrial production. In addition, the process conditions were screened and the best reaction conditions were determined.
- 【文献出处】 广州化工 ,Guangzhou Chemical Industry , 编辑部邮箱 ,2024年09期
- 【分类号】TQ465
- 【下载频次】2