新型奥美拉唑合成及质子泵抑制剂药物杂质研究进展

S. Saini, C. Majee, G. Chakraborthy, Salahuddin
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引用次数: 2

摘要

摘要:本文综述了质子泵抑制剂中奥美拉唑合成及药物杂质的新方法,为质子泵抑制剂的开发提供参考。然而,本文着重于抗溃疡药物中各种药物杂质的研究。研究中使用的药物是奥美拉唑,化学上称为(5-甲氧基-2-[[(4-甲基-3,5二甲基吡啶基)甲基]亚砜基]-l-苯并咪唑),通过氧化其巯基来抑制胃atp酶。合成过程合成过程中所涉及的过程该新工艺是由于吡甲唑不完全氧化和过氧化生成砜而形成n -氧化物砜而产生的。该过程涉及5-甲氧基噻吩并咪唑形成酯,然后将酯与格氏试剂2-氯甲基-4-甲氧基-3,5-二甲基吡啶偶联。本发明的合成药物杂质的新工艺达到了预期的产率,且过程短、简单。合成的质子泵抑制剂杂质可作为标准杂质,用于各方面的进一步研究。这篇综述文章将介绍奥美拉唑在市场上销售的各种新的杂质。
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Novel Synthesis of Omeprazole and Pharmaceutical Impurities of Proton pump inhibitors : A Review
Abstract : The objective of this review was to study the novel methods to the omeprazole synthesis and pharmaceutical impurities of proton pump inhibitors that provide an insight to researchers about the development of proton pump inhibitors. However, this paper emphasized on the study of various pharmaceutical impurities of anti-ulcer drug. The drug used for the study was omeprazole which is chemically known as (5-methoxy-2-[[(4-metboxy-3,5dimethylpyridinyl) methyl] sulfinyl]-l-benzimidazole) that inhibits gastric ATPase enzyme by oxidizingits sulfhydryl groups.The process involved during synthesis. The novel process come into existence due to incomplete oxidation of pyrmetazole and overoxidation to sulfone that leads to the formation of sulfone N-oxide. The procedure involved 5-methoxy thiobenzimidazole to the formation of an ester followed by coupling of the ester with the Grignard reagent of 2-chloromethyl-4-methoxy-3,5-dimethyl-pyridine. The novel synthesis process for pharmaceutical impurities achieve the expected yield and process observed to be short, simple. The synthesized impurity of proton pump inhibitors can be used as standard impurity, that can be utilized for further studied in various aspects. This review article will describe about the various novel impurities of omeprazole that available as marketed formulation.
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