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非阿片类止痛药氟吡汀马来酸盐的制备及晶型调控和表征
Synthesis and modification transformation and characterization of non-opiate analgesic flupirtine maleate
【Author】 MENG Qing-wei, ZHOU Yu-yu, LIU Jun, ZHAO Wei-jie (Department of Chemical Engineering, Dalian University of Technology, Dalian 116024, China)
【机构】 大连理工大学化工学院；
【摘要】 氟吡汀马来酸盐是以2,6-二氯-3-硝基吡啶为原料,分别与氨,对氟苄胺在2,6位发生取代,硝基的加氢还原,接着与氯甲酸乙酯发生酰化反应,再与马来酸成盐来制备。总收率76．5％, 晶型为B型,在异丙醇溶剂20C,180rm搅拌条件下,分别在1h、1．5h、2．0h、3．0h用小角X衍射仪检测其晶型为11％A,22％A,42％A,85％A的混合晶型,对其不同混合晶型的DSC(差热分析) 曲线进行了研究,得出A,B两种晶型的特征峰的变化规律,并测定并比较了两种晶型抗自由基活性。
【Abstract】 Amination at position 2,6 of the raw material 2,6-dichloro-3-nitropyridine, respectively by ammonia and 4-fluorobenzylamine, followed by hydrogenation and acylation at position 3 gave Flupirtine, whose maleate is an analgesic drug without dependence. Various crystal modifications formed were analyzed by DSC and examined by X-ray diffractometry. It is shown how to obtain the modification wanted by DSC monitoring and the little difference in anti-free-radicals between the two modification A,B.
【Key words】 flupirtine maleate； modification； preparation； x-ray diffratometry； thermoanalysis； anti-free radical；
- 【会议录名称】 大连理工大学生物医学工程学术论文集（第2卷）
- 【会议名称】大连理工大学生物医学工程学会研讨会
- 【会议时间】2005-12
- 【会议地点】中国辽宁大连
- 【分类号】TQ463.53
- 【主办单位】大连理工大学