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Synthesis of 4-((1H-benzo[d]imidazol-2-yl)oxy)-3-methylpicolinic acid, a key related substance of Rabeprazole sodium
Tetrahedron Letters ( IF 1.8 ) Pub Date : 2020-06-02 , DOI: 10.1016/j.tetlet.2020.152105
Xiaoyan He , Yan Chang , Xuefei Bao , Zi'ao Liu , Guoliang Chen , Xiuhong Lu

4-((1H-benzo[d]imidazol-2-yl)oxy)-3-methylpicolinic acid (11) is a key related substance of Rabeprazole sodium. In this article, this key related substance is synthesized by using 3-methylpicolinonitrile as a starting material via a five-step processes. By converting 3-methylpicolinonitrile to 4-hydroxy-3-methylpicolinonitrile (13), the preparation of TM becomes practical. This work provides a guarantee for quality standard establishment of Rabeprazole sodium.



中文翻译:

雷贝拉唑钠的关键相关物质4-((1 H-苯并[ d ]咪唑-2-基)氧基)-3-甲基吡啶甲酸的合成

4-((1 H-苯并[ d ]咪唑-2-基)氧基)-3-甲基吡啶甲酸(11)是雷贝拉唑钠的关键相关物质。在本文中,该关键相关物质是使用3-甲基吡啶啉作为起始原料通过五步法合成的。通过将3-甲基吡啶甲基腈转化为4-羟基-3-甲基吡啶甲基腈(13),TM的制备变得可行。这项工作为建立雷贝拉唑钠的质量标准提供了保证。

更新日期:2020-07-05
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