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美罗培南脱保护工艺改进

Improvement of the deprotection of Meropenem
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摘要 采用Zn粉/KH_2PO_4代替钯碳/H_2催化氢化体系,脱去保护的美罗培南的保护基对硝基苄基(PNB)、对硝基苄氧羰基(PNZ),得到美罗培南,收率达92%.最佳反应条件为:以THF/H_2O为溶剂,Zn粉4.0g,KH_2PO_43.0g,在30℃下反应3.5h.其结构经核磁共振氢谱(~1H NMR)确认. By using zinc powder/KH2PO4 instead of palladium carbon/H2 catalytic system, p-nitro- benzyl (PNB) and p-nitrobenzyloxycarbonyl (PNZ) the protecting group can be removed from meropenem ester to obtain meropenem with an overall yield of up to 92 %. Optimum reaction conditions are as follows, with THF/H20 as solvent, 4.0g zinc powder as catalyst, 3.0g KH2PO4, reacting for 3.5 h under 30℃, the target compound structure is confirmed by 1HNMR.
出处 《石家庄职业技术学院学报》 2017年第4期32-34,43,共4页 Journal of Shijiazhuang College of Applied Technology
关键词 Zn粉 催化氢化 脱保护 美罗培南 zinc powder catalytic hydrogenation deprotection meropenem
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