| 厄贝沙坦的合成 |
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| 引用本文： | 岑均达,马霞.厄贝沙坦的合成[J].中国医药工业杂志,2007,38(3):239-240. |
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| 作者姓名： | 岑均达 马霞 |
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| 作者单位： | 上海医药工业研究院,上海,200437 |
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| 摘 要： | 环戊酮与氰化钠反应制得1-氨基环戊腈，成盐、水解成酰胺后与戊酰氯反应制得2-丁基-1，3-二氮杂螺4-4]壬-1-烯-4-酮，相转移催化条件下与4’-溴甲基-2-氰基联苯反应制得2-丁基-3-（2’-氰基联苯-4-基）甲基]-1，3-二氮杂螺4-4]壬-1-烯-4-酮，最后与叠氮化钠反应制得厄贝沙坦，总收率约39％。
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| 关 键 词： | 厄贝沙坦 血管紧张素Ⅱ受体拮抗剂 抗高血压药 相转移催化 合成 |
| 文章编号： | 1001-8255（2007）03-0239-02 |
| 修稿时间： | 2006-10-08 |
Synthesis of Irbesartan |
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| Authors: | CEN Jun-da MA Xia |
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| Institution: | Shanghai Institute of Pharmaceutical Industry, Shanghai 200437 |
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| Abstract: | Cyclopentanone was reacted with sodium syanide,followed by hydrolysis to afford the amide, which was condensed with valeryl chloride,and then reacted with 4'-(bromomethyl)-2-cyanobiphenyl under phase transfer condition to give 2-butyl-3-(2'-cyanobiphen-4-yl)methyl]-1,3-diazaspiro4,4]non-1-en-4-one.Finally,the latter was cyclized with sodium azide to afford the antihypertensive agent irbesartan with overall yield of 39%,based on cyclopentanone. |
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