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Synthesis of benzoyl ornidazole

2011 
The invention relates to a new method for synthesizing an ornidazole derivative, namely benzoyl ornidazole. At present, ornidazole is a third-generation novel nitroimidazole derivative after metronidazole and tinidazole, has high anaerobe resistance and protozoan resistance, but is difficultly applied to children because of bitter taste. The invention aims to provide a new method for synthesizing the ornidazole derivative. The synthesis method comprises the following steps of: adding ornidazole, fatty acid and fatty alcohol ester, and aliphatic tertiary amine or nitrogen heterocycle organic base in turn, stirring for dissolution and clarification, heating to refluxing temperature, dripping benzoyl chloride, and reacting by keeping temperature under normal pressure; cooling, adding water, stirring, standing for demixing, adding water to wash an organic phase, cooling and freezing for crystallization, filtering, washing, and drying to obtain a crude product; and recrystallizing the crude product by using ethanol to obtain the benzoyl ornidazole. The method has the advantages that: the obtained benzoyl ornidazole is a precursor medicine of ornidazole, the original bitter taste of the ornidazole is eliminated, and a method for industrially producing the benzoyl ornidazole is realized.
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