| 咪唑斯汀的生产工艺改进 |
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| 引用本文： | 王群方,王子寒. 咪唑斯汀的生产工艺改进[J]. 浙江化工, 2014, 0(10): 4-6 |
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| 作者姓名： | 王群方 王子寒 |
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| 作者单位： | 贝达药业股份有限公司;西北师范大学 |
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| 摘 要： | 首先以4-氟苄基氯和2-氯-1H-苯并咪唑为起始原料合成1-[（4-氟苯基）甲基]-2-氯-1H-苯并咪唑中间体;所得中间体进一步与甲胺哌啶反应得1-[1-（4-氟苄基）甲基-1H-苯并咪唑-2-基]-N-甲基-4-哌啶胺;最后,第二步产物进一步与2-甲硫基-4-嘧啶酮反应制得（2-[[1-[1-（4-氟苄基）-1H-苯并咪唑-2-基]-4-哌啶基]甲胺基]-4（1H）-嘧啶酮）（咪唑斯汀）,总生产收率达54%。
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| 关 键 词： | 咪唑斯汀 生产工艺 抗过敏 |
Improvement on the Production Process of Mizolastine |
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| WANG Qun-fang;WANG Zi-han. Improvement on the Production Process of Mizolastine[J]. Zhejiang Chemical Industry, 2014, 0(10): 4-6 |
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| Authors: | WANG Qun-fang WANG Zi-han |
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| Affiliation: | WANG Qun-fang;WANG Zi-han;Zhejiang Betta Pharmaceuticals Co., Ltd.;Northwest Normal University; |
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| Abstract: | Firstly, 1-（4-Fluorobenzyl）-2-chloro-1H-benzoimidazole was synthesized from 4-fluorobenzyl chloride and 2-chloro-1H-benzimidazole. Secondly, the obtained 1-（4-Fluorobenzyl）-2-chloro-1H-benzoimidazole ammonolysis reacted with methylamine piperidine to give 1-[1-（4-fluoro-benzyl）methyl-1H-benzimidazol-2-yl]-N-methyl-4– piperidinamine. Finally, mizolastine was synthesized from 1-[1-（4-fluoro-benzyl）methyl-1H-benzimidazol-2-yl]-N-methyl-4-piperidinamine and 2-methylthio-4-pyrimidone.The overall yield was about 54%. |
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| Keywords: | mizolastine production process antiallergic |
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