利奈唑酮的合成研究

Studies on synthesis of linezolid

以3,4-二氟硝基苯为起始原料,经取代、硝基还原、酰化、环合、磺化、叠氮化、叠氮基还原及乙酰化反应合成利奈唑酮。产物结构经过了IR和1 HNMR的确证。重点研究了取代反应的缚酸剂、催化加氢还原硝基的溶剂、叠氮的亚磷酸三甲酯还原反应,确定了最佳反应条件,以总收率49.8%合成了目标产物。

Linezolid has been synthesized from the 3,4-difluoronitrobenzene through substitution,nitro reduction,acylation,condensation,sulfonation,azide,azide group reduction and acylation with acetic anhydride.The chemical structure of the product was identified by IR and 1 H NMR.The optimal reaction conditions were investigated,including substitution,nitro reduction and azide group reduction.Linezolid was synthesized with the total yield of 49.8%.