异环型双膦酸类药物唑来膦酸合成新工艺研究  

Study on the novel process for preparation of zoledronic acid

作　　者：董华青[1] 高建荣[1] 贾建洪[1] 徐时良[1] 

机构地区：[1]浙江工业大学化学工程与材料学院,浙江杭州310032

出　　处：《浙江工业大学学报》2008年第2期141-143,154,共4页Journal of Zhejiang University of Technology

摘　　要：研究了以咪唑和氯乙酸乙酯为原料经相转移催化N-烷基化反应、水解、成盐制得咪唑乙酸盐酸盐,再与三氯氧磷和亚磷酸反应后水解合成唑来膦酸的新工艺.通过工艺优化,在较佳工艺条件下反应总收率达53%,纯度达99%.新工艺具有反应时间短、产品纯度和收率高及操作简便等特点.用IR,1H NMR及MS确证了唑来膦酸的结构.Zoledronic acid was prepared from imidazole by the reactions of phase transfer catalysis N-alkylation with ethyl chloroacetate, salification and hydrolysis. Under the optimal conditions, the overall yield of zoledronic acid is 53% with the purity of 99%. The novel process features short reaction time, moderate yield and simple workup. The structure of zoledronic acid was confirmed by IR, 1HNMR and MS.

关 键 词：唑来膦酸 相转移催化 N-烷基化 工艺优化 

分 类 号：TQ126.3[化学工程—无机化工]