摘要
目的制备新型磷结合剂比沙洛姆并优化其合成工艺。方法以1,4-丁二胺为起始原料,经加成、氢化、共聚反应得到目标物比沙洛姆。结果与结论目标物比沙洛姆的结构经固体核磁共振氢谱和碳谱、红外光谱分析、元素分析、X-粉末衍射谱、扫描电镜图谱确证。改进后的合成工艺条件温和、操作简便、成本低、产品质量稳定,路线总收率79.1%,适合工业化生产。
Bixalomer is a novel non aluminum,non calcium phosphorus binder,applied to improve hyperphosphatemia of dialysis patients with chronic renal failure.There was only one synthetic route reported in the recent literature.By using 1,4-butanediamine as the starting material,bixalomer was prepared through addition,hydrogenation and copolymerization.In order to obtain a synthetic route with mild reaction conditions,simple operation and environmental protection,the novel route adjusted the material ratio,used of methanolamine instead of active nickel.The reaction temperature and the workup method were improved and the refining was removed.The solvent and catalyst were investigated in the hydrogenation reaction.The diluted hydrochloric acid was proved suitable for the copolymerization.The synthetic route was optimized and more suitable for industrial production.The structure of target compound was confirmed by solid state NMR,infrared spectra,elemental analysis,XRD and SEM.
作者
司鸽
张代铭
王剑平
吴辉
郑忠辉
SI Ge;ZHANG Dai-ming;WANG Jian-ping;WU Hui;ZHENG Zhong-hui(Zibo Vocational Institute,Zibo 255314,China;Shandong Xinhua Pharmaceutical Co.,Ltd.,Zibo 255086,China)
出处
《中国药物化学杂志》
CAS
CSCD
北大核心
2020年第7期419-422,共4页
Chinese Journal of Medicinal Chemistry
关键词
比沙洛姆
化学合成
高磷血症治疗剂
磷酸结合聚合物
bixalomer
chemical synthesis
treatment for hyperphosphatemia
phosphate binding polymer
