1-(2,5-二甲氧基苯基)-2-氨基乙醇的合成进展
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摘要
盐酸米多君是由奥地利Chemie Linz公司研制的一种前体药,并经酶促水解,代谢为药理学上有活性物质脱甘氨酸米多君。脱甘氨酸米多君选择性地刺激外周a-肾上腺素能受体。此药对心肌β-肾上腺素能受体无作用。其他作用基本相当于其他似a-交感神经药的作用。在此药的作用下,收缩压均升高,并出现反射性心动过缓。该药已在德、美等欧洲国家上市。中国目前也有药企的仿制药在国内上市。本文对盐酸米多君中间体1-(2,5-二甲氧基苯基)-2-氨基乙醇1的合成方法进行了综述,以期为该药物的合成及工业化生产提供参考。
Midodrine hydrochloride is one kind of prodrug developed by Austria Chemie Linz company and after the enzymatic hydrolysis, it is metabolized to Midodrine Related Compound A. The Midodrine Related Compound A stimulates selectively peripheral a-adrenoceptor. This medicine has no function on myocardium β-adrenoceptor and its other functions is basically similar to the function of a-sympathetic nerve medicine. Under the function of this medicine, the systolic pressure increases with reflexive bradycardia. This medicine has already appeared on the markets of Germany, America etc., European countries. Currently, China also has the generic medicine of pharmaceutical company on domestic market. This paper, has summarized the synthesis method of the intermediate,1-(2,5-dimethoxyphenyl)-2-amidogen ethyl alcohol 1 of midodrine hydrochloride so that to provide reference of its synthesis and industrialized production.
Midodrine hydrochloride is one kind of prodrug developed by Austria Chemie Linz company and after the enzymatic hydrolysis, it is metabolized to Midodrine Related Compound A. The Midodrine Related Compound A stimulates selectively peripheral a-adrenoceptor. This medicine has no function on myocardium β-adrenoceptor and its other functions is basically similar to the function of a-sympathetic nerve medicine. Under the function of this medicine, the systolic pressure increases with reflexive bradycardia. This medicine has already appeared on the markets of Germany, America etc., European countries. Currently, China also has the generic medicine of pharmaceutical company on domestic market. This paper, has summarized the synthesis method of the intermediate,1-(2,5-dimethoxyphenyl)-2-amidogen ethyl alcohol 1 of midodrine hydrochloride so that to provide reference of its synthesis and industrialized production.
引文
[1]孟庆玉,肖方青,刘旭桃,高云等.盐酸米多君的合成[J].中国医学杂志,2002,33(5):213-215.
[2]宋洪海,覃湘东,刘小东,牛子霞,郭心富等.盐酸米多君中间体1-(2,5-二甲氧基苯基)-2-氨基乙醇的制备方法[P].中国专利,102060719,2011-05-28.
[2]宋洪海,覃湘东,刘小东,牛子霞,郭心富等.盐酸米多君中间体1-(2,5-二甲氧基苯基)-2-氨基乙醇的制备方法[P].中国专利,102060719,2011-05-28.