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枸橼酸托瑞米芬的合成工艺优化研究

Study on optimization of synthetic process of toremifene citrate
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摘要 枸橼酸托瑞米芬的化学名为Z-2-[4-(4-氯-1,2-二苯基)-1-丁烯基]苯氧基]-N,N-二甲基乙胺单枸橼酸盐,是一类非甾体抗雌激素类抗肿瘤药物,可以对乳腺癌进行治疗。主要针对枸橼酸托瑞米芬的合成工艺进行分析,并针对工艺优化进行了相关实验。采用的实验方法为,以4-羟基二苯甲酮为原料,并经过缩合、还原、氯代以及成盐等反应,合成枸橼酸托瑞米芬。根据实验结果可以发现,枸橼酸托瑞米芬的反应总收率达到60.0%,并对其产物采用红外光谱、高分辨质谱以及核磁共振等进行表证。该工艺反应温和、简单,具有污染小、纯度好以及收率高等特点,适合在工业化生产当中进行应用。 Toromifene citrate is chemically named Z-2-[4-(4-chlorine-1,2-two phenyl)-1-butenyl]phenoxy]-N,N-two methyl ethylamine mono citrate.It is a kind of non steroidal anti estrogen antitumor drug which can be used for the treatment of breast cancer.The synthetic process of toremifene citrate was analyzed,and the related experiments were carried out for the process optimization.Toremifene citrate was synthesized from 4-hydroxybenzophenone through condensation,reduction,chlorination and salt formation.According to the experimental results,it was found that the total yield of toremifene citrate was 60.0%,and the products were confirmed by IR,HRMS and NMR.The process has the characteristics of mild and simple reaction,low pollution,good purity and high yield.It is suitable for industrial production.
作者 范子祺 FAN Ziqi(Nanjing Weikaier Biomedical Technology Co.,Ltd.,Nanjing Jiangsu 211100,China)
出处 《山西化工》 2022年第1期19-21,共3页 Shanxi Chemical Industry
关键词 枸橼酸托瑞米芬 合成工艺 优化对策 实验研究 toremifene citrate synthesis process optimization countermeasures experimental study
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