帕尼培南关键中间体2-酮碳青霉烷-3-羧酸对硝基苄酯的合成改进

目的 合成帕尼培南关键中间体(3R,5R,6S)-6-(1R)-羟乙基]碳青霉烷-2酮-3-羧酸对硝基苄酯。方法 以对硝基苯甲醛为起始原料，经还原、酯化、重氮化、烯醇化、与单环β-内酰胺结合、水解及环合等7步反应制得目标化合物。结果与结论 合成的目标化合物经IR、¹H-NMR、MS确证结构，总收率达60.7 %。该合成工艺省去文献中两步需要分离纯化的步骤，使合成路线大为简化。

Improved synthesis of the panipenem intermediate p-nitrobenzyl -2-oxo-carbapenam-3-carboxylate

Aim To synthesize a panipenem intermediate, p-nitrobenzyl (3R,5R,6S)-2-oxo-6-(1R)-1- hydroxyethyl]carbapenam-3-carboxylate. Methods Commercially available 4-nitrobenzaldehyde was used as starting material to give target compound via reduction, esterification, diazotization, enolization, condensation, hydrolysis, and cyclization. Results and conclusion The target compound was prepared in 60.7 % overall yield and its structure was identified by IR, ¹H-NMR and MS.