美罗培南脱保护工艺改进  

Improvement of the deprotection of Meropenem

作　　者：王玉芳[1] 孙百虎[2] 于海军[1] 

机构地区：[1]石家庄职业技术学院科技发展与校企合作部,河北石家庄050081 [2]石家庄职业技术学院教务处,河北石家庄050081

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

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.

关 键 词：Zn粉 催化氢化 脱保护 美罗培南 

分 类 号：TQ465[化学工程—制药化工]