利奈唑胺制备工艺的优化研究

Optimization of the Preparation of Linezolid

以吗啉和3,4-二氟硝基苯为原料,通过缩合、还原、环合、肼解、和酰化反应制备利奈唑胺,优化了合成工艺中还原反应和环合反应步骤:在还原反应中,用氢气还原代替甲酸铵做氢源;在环合反应中,用固体光气代替光气反应构建噁唑烷酮,并优化固体光气的反应温度对反应的影响,确定了最佳反应条件,总收率达65.2%,产品结构经~1HNMR、ESI-MS确证。

With morphpline and 3,4-difluoronitrobenzene as raw material,linezolid was obtained through condensation,reduction,cyclization,hydrazinolysis,and acylation. The steps of reduction and cyclization reaction in the synthesis reaction were optimized： in the reduction,hydrogen was used as a source of ammonium formate; in cyclization reaction,triphosgene was used in place of phosgene to form oxazolidinone. The effects of material and temperature on the reaction were explored and the optimum reation conditions were determined. The total yield was 65. 2% and the product structure was determined by ^1HNMR,ESI-MS.