| 对胍基苯甲酸盐酸盐的制备及衍生物卡莫他特甲磺酸盐的合成 |
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| 引用本文： | 王晓天,张建宾,金汝城. 对胍基苯甲酸盐酸盐的制备及衍生物卡莫他特甲磺酸盐的合成[J]. 精细化工, 2004, 21(8): 597-599 |
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| 作者姓名： | 王晓天 张建宾 金汝城 |
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| 作者单位： | 天津大学,药学院,天津,300070;天津药物研究院,化学制药研究部,天津,300193 |
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| 摘 要： | 以对氨基苯甲酸为起始原料,水浴加热至50℃,与单氰胺进行反应,然后加入w(HCl)=5%的水溶液使产品析出,一步合成对胍基苯甲酸盐酸盐(收率为76 4%);它与对羟基苯乙酸N,N 二甲基氨基甲酰甲酯在25℃、二环己基碳二亚胺(DCC)存在下酯化缩合,再转化成碳酸盐进行精制,所得产物和水形成的悬浮液用甲磺酸调pH=3,得到卡莫他特甲磺酸盐(总收率为64 4%)。操作简单,原料易得,条件温和,有工业化前景。
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| 关 键 词： | 顶体蛋白酶抑制剂 对胍基苯甲酸 卡莫他特甲磺酸盐 |
| 文章编号： | 1003-5214(2004)08-0597-03 |
Synthesis of p-Guanidinobenzoic Acid Hydrochloride and Its Derivative Camostat Mesylate |
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| WANG Xiao-tian,ZHANG Jian-bin,JIN Ru-cheng. Synthesis of p-Guanidinobenzoic Acid Hydrochloride and Its Derivative Camostat Mesylate[J]. Fine Chemicals, 2004, 21(8): 597-599 |
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| Authors: | WANG Xiao-tian ZHANG Jian-bin JIN Ru-cheng |
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| Affiliation: | WANG Xiao-tian~1,ZHANG Jian-bin~2,JIN Ru-cheng~1 |
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| Abstract: | p -Aminobenzoic acid is stirred with cyanamide in water-bath at 50 ℃,and then aqueous HCl 〔 w (HCl)=5%〕 is dropped to precipitate p -guanidinobenzoic acid hydrochloride(Ⅰ) in 76 .4% yield.In the presence of DCC ( N,N ′-dicyclohexylcarbodiimide),Ⅰ reacts at first at room temperature (25 ℃) with N,N -dimethylcarbamoylmethyl p -hydroxyphenylacetate,then the product is purified by changing it to carbonic salt,at last methanesulfonic acid is added to adjust pH to 3 to give camostat mesylate in 64 .4% yield.This method is simple,and the materials are easy to get.It is significant for industrial production. |
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| Keywords: | acrosin inhibitor p -guanidinobenzoic acid camostat mesylate |
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