| 新型抗前列腺增生药物度他雄胺的合成 |
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| 引用本文： | 梁涌涛,徐志炳,路海滨,王恩思.新型抗前列腺增生药物度他雄胺的合成[J].吉林大学学报(理学版),2007,45(6):1035-1038. |
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| 作者姓名： | 梁涌涛 徐志炳 路海滨 王恩思 |
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| 作者单位： | 1. 吉林大学 生命科学学院, 长春 130021； 2. 吉林大学 药学院, 长春 130021 |
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| 摘 要： | 以孕烯酮酸为原料, 采用碳 17位上羧基的酰胺化为关键步骤, 以DDQ/BSTFA为氧化剂进行1,2位脱氢合成度他雄胺, 总收率为23%. 关键中间体和度他雄胺的结构经红外光谱、 核磁共振氢谱及碳谱、 质谱等得到确证.
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| 关 键 词： | 合成 度他雄胺 药物化学 抗前列腺增生药物 |
| 文章编号： | 1671-5489（2007）06-1035-04 |
| 收稿时间： | 2007-03-23 |
| 修稿时间： | 2007-03-23 |
Synthesis of Anti-benign Prostatic Hyperplasia Drug Dutasteride |
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| LIANG Yong-tao,XU Zhi-bing,LU Hai-bin,WANG En-si.Synthesis of Anti-benign Prostatic Hyperplasia Drug Dutasteride[J].Journal of Jilin University: Sci Ed,2007,45(6):1035-1038. |
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| Authors: | LIANG Yong-tao XU Zhi-bing LU Hai-bin WANG En-si |
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| Institution: | 1. College of Life Science, Jilin University, Changchun 130021, China; 2. College of Pharmacy, Jilin University, Changchun 130021, China |
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| Abstract: | Dutasteride, a new kind of anti benign prostatic hyperplasia drug, 17-β-N (2,5-bis(trifluoromethyl)) phenylcarbamoyl-4-aza-5-α-androst-1-en-3-one, was synthesized by employing amidation and DDQ/BSTFA oxidation as a pivotal step from the starting material 3-oxo-4-androstene-17-β-carboxylic acid. The total yield of dutasteride synthesi
zed was 23%. The structures of the target molecule and the key intermediates were confirmed by IR,1H NMR, 13C NMR and MS. The route does not require high pressure and high temperature that may be applied to industrial production. |
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| Keywords: | synthesis dutasteride medicinal chemistry anti-benign prostatic hyperplasia drug |
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