| 2-甲氧基雌二醇合成方法的改进 |
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| 引用本文： | 张蓓娜,王宏博,张倩,陈瑛,夏鹏.2-甲氧基雌二醇合成方法的改进[J].复旦学报(医学版),2003,30(5):494-495. |
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| 作者姓名： | 张蓓娜 王宏博 张倩 陈瑛 夏鹏 |
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| 作者单位： | 复旦大学药学院药物化学教研室,上海,200032 |
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| 摘 要： | 目的 合成抗肿瘤新药新生血管形成抑制剂2-甲氧基雌二醇。方法 以雌二醇为原料经2一位溴代，继而甲氧基化直接合成2-甲氧基雌二醇。结果 改进的合成方法割除了文献报道方法中的3，17-双乙酰化及水解二个反应步骤，合成获得的2-甲氧基雌二醇成品进行了结构确证。结论 通过有效地纯化2-溴雌二醇中间体，可缩短二步反应直接制得成品。
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| 关 键 词： | 2-甲氧基雌二醇 合成方法 抗肿瘤药 2-溴雌二醇 中间体 雌二醇 |
| 修稿时间： | 2002年11月18 |
An Improved Synthetic Method of 2-Methoxyestradiol |
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| ZHANG Bei-na,WANG Hong-bo,ZHANG Qian,CHEN Ying,XIA Peng.An Improved Synthetic Method of 2-Methoxyestradiol[J].Fudan University Journal of Medical Sciences,2003,30(5):494-495. |
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| Authors: | ZHANG Bei-na WANG Hong-bo ZHANG Qian CHEN Ying XIA Peng |
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| Abstract: | Purpose To synthesize a new antitumor drug 2-methoxyestradiol which is an angiogenesis inhibitor. Methods 2-methoxyestradiol was directly synthesized by 2-bromination followed methoxylation from estradiol. Results Compared with reported method,two reaction stages (3,17-diacetylation and hydrolysis) were omitted in improved synthesis.The structure of obtained 2-methoxyestradiol was confirmed via 1H?NMR and mass spectrum. Conclusions The two reaction stages in reported synthetic procedure of 2-methoxyestrdiol can be shortened via efficient purification of 2-bromoestradiol intermediate. |
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| Keywords: | methoxyestradiol estradiol angiogenesis inhibitor 4-methoxyestradiol |
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