| 4-(1-羟基-1-甲基乙基)-2-丙基-1H-咪唑-5-羧酸乙酯的合成 |
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| 引用本文： | 卫禾耕,王平,郑国君,李毅,吴迎秋. 4-(1-羟基-1-甲基乙基)-2-丙基-1H-咪唑-5-羧酸乙酯的合成[J]. 中国医药工业杂志, 2012, 43(1): 14-16 |
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| 作者姓名： | 卫禾耕 王平 郑国君 李毅 吴迎秋 |
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| 作者单位： | 1. 浙江海正药业有限公司,浙江台州,318000
2. 东北农业大学生物化学工程系,黑龙江哈尔滨,150030 |
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| 摘 要： | 2-甲基-2-羟基丙腈(2)经三甲基硅基(TMS)保护后,经Blaise反应并脱三甲基硅烷基保护,在亚硝酸钠和乙酸作用下肟化和Pd/C催化还原得到2-氨基-4-羟基-4-甲基-3-氧代戊酸乙酯三氟乙酸盐,再与丁酰亚氨酸甲酯盐酸盐环合得到奥美沙坦酯关键中间体4-(1-羟基-1-甲基乙基)-2-丙基-1H-咪唑-5-羧酸乙酯,总收率约40%。
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| 关 键 词： | 4-(1-羟基-1-甲基乙基)-2-丙基-1H-咪唑-5-羧酸乙酯 奥美沙坦酯 抗高血压药 中间体 合成 |
Synthesis of Ethyl 4- (1-Hydroxy- 1-methylethyl) -2-propyl-4,5-dihydro-1H-imidazole-5-carboxylate |
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| WEI Hegeng , WANG Ping , ZHENG Guojun , LI Yi , WU Yingqiu. Synthesis of Ethyl 4- (1-Hydroxy- 1-methylethyl) -2-propyl-4,5-dihydro-1H-imidazole-5-carboxylate[J]. , 2012, 43(1): 14-16 |
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| Authors: | WEI Hegeng WANG Ping ZHENG Guojun LI Yi WU Yingqiu |
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| Affiliation: | 1(1.Zhejiang Hisun Pharmaceutical Co.,Ltd.,Taizhou 318000;2.Dept.of Biochemical Engineering,Northeast Agricultural University,Harbin 150030) |
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| Abstract: | Ethyl 4-(1-Hydroxy-1-methylethyl)-2-propyl-4,5-dihydro-1H-imidazole-5-carboxylate,a key intermediate of olmesartan medoxomil,was synthesized from 2-hydroxy-2-methylpropanenitrile by protection with trimethylsilyl,Blaise reaction,deprotection,oximation with sodium nitrite and acetic acid,reduction with Pd/C as catalyst and cyclization with methyl butanimidate hydrochloride with an overall yield of about 40%. |
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| Keywords: | ethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-4,5-dihydro-1H-imidazole-5-carboxylate olmesartan medoxomil antihypertensive intermediate synthesis |
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