利奈唑胺合成工艺的优化

Optimization of synthetic process of Linezolid

利奈唑胺是新型化学全合成噁唑烷酮类抗菌药,本文通过研究对比,首先合成(S)-N-[2-(乙酰氧基)-3-氯丙基]乙酰胺和N-羰基苄氧-3-氟-4-吗啉基苯胺,利用缩合反应制备利奈唑胺的方法,经过一系列地优化,发现了适合工业化生产的工艺路线。

Linezolid is a novel chemical synthesis of oxazolidinone antibacterial drugs. This paper compared these reported literature and optimized its synthetic route. First, synthesis of （S）-N-[2 - （acetylaminooxy） -3 - chloropropyl] acetamide and N-carbonyl-benzyloxycarbonyl -3 - fluoro-4 - morpholinyl aniline, then by using the condensation reaction method of the above key intermediates to get high quality linezolid, after a series of optimization, a promising industrialization production process route was established.