| 枸橼酸托瑞米芬的中间体合成工艺改进 |
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| 引用本文： | 张瑞仁,刘红,祝红兵,王旭. 枸橼酸托瑞米芬的中间体合成工艺改进[J]. 黑龙江医药科学, 2012, 35(4): 29-30 |
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| 作者姓名： | 张瑞仁 刘红 祝红兵 王旭 |
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| 作者单位： | 佳木斯大学药学院,黑龙江佳木斯,154007 |
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| 摘 要： | 目的:研究了抗肿瘤药物枸橼酸托瑞米芬的中间体1,2-二苯基-1-[4-[2-(N,N-二甲胺基)乙氧苯基]]-1,4-丁二醇的合成工艺改进。方法:以4-羟基二苯甲酮为原料经过取代与加成两步反应合成了目标物,并进行工艺的优化实验。结果:中间体合成工艺得到改进和优化,两步收率合计55.4%。结论:研究出了一条生产成本低,反应温和,操作简单的枸橼酸托瑞米芬的中间体合成工艺。
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| 关 键 词： | 1,2-二苯基-1-[4-[2-(N,N-二甲氨基)乙氧苯基]]-1,4-丁二醇 肉桂醇 托瑞米芬 抗肿瘤药物 |
Improvement on the synthesis of an intermediate for toremifene citrate |
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| ZHANG Rui-ren , LIU Hong , ZHU Hong-bing , WANG Xu. Improvement on the synthesis of an intermediate for toremifene citrate[J]. Heilongjiang Medicine and Pharmacy, 2012, 35(4): 29-30 |
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| Authors: | ZHANG Rui-ren LIU Hong ZHU Hong-bing WANG Xu |
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| Affiliation: | ZHANG Rui-ren,LIU Hong,ZHU Hong-bing,WANG Xv(College of Pharmacy of Jiamusi University,Jiamusi 154007,China) |
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| Abstract: | Objective: To synthesize a key intermediate of antineoplastic drug,1,2-dibenzyl-1-[4-[2-(N,N-dimethylamino)ethoxyl]phenyl]-butane-1,4-diol.Methods: The intermediate was synthesized with 4-hydroxydiphenyl ketone as raw materials,by substitution reaction and addition reaction.Results:The intermediate has been optimized and improved.The overall yield is 55.4%.Conclusion:The mild and easy synthesis process,which has a lower cost,has been worked out. |
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| Keywords: | 1,2-dibenzyl-1-[4-[2-(N,N-dimethylamino)ethoxyl]phenyl]-butane-1,4-diol cinnamyl alcohol toremifene citrate antineoplastic |
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