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罗氟司特N-氧化物的合成与晶型研究

Synthesis and polymorphic study of roflumilast N-oxide

  • 摘要: 对罗氟司特在体内的活性代谢物罗氟司特N-氧化物的合成进行了工艺改进,总收率为19%。通过X线粉末衍射、红外光谱、差示扫描量热分析及元素分析等方法确定了罗氟司特N-氧化物的晶型物Ⅰ和晶型物Ⅱ,并测定了一水合晶型物Ⅱ的X线单晶衍射结构。

     

    Abstract: This paper describes a practical process for the preparation of an active metabolite of roflumilast,with an overall yield of 19%.The polymorphic substances of roflumilast N-oxide were characterized by means of X-ray powder diffraction,IR,DSC,TGA and elemental analysis.Roflumilast N-oxide was found to exist in two crystal forms,form I and monohydrate form II Monohydrate crystal form II was further indentified by single-crystal X-ray structure analysis.

     

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