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    • 55. 发明授权
    • Method for preparation of cefuroxime axetil
    • 头孢呋辛酯的制备方法
    • US07064198B2
    • 2006-06-20
    • US10468584
    • 2001-07-25
    • Vinod Kumar KansalSunil Gurudatt BhatTanguturi Venkata MarutikumarYuvaraj Atmaram ChavanRamanathan Sankaran
    • Vinod Kumar KansalSunil Gurudatt BhatTanguturi Venkata MarutikumarYuvaraj Atmaram ChavanRamanathan Sankaran
    • C07D501/34C07D501/04
    • C07D501/00
    • A process for preparation of cefuroxime axetil of formula (I) of at least 96% purity and substantially free of analogous Δ2-isomer of formula (II) and other impurities. The process comprises reacting cefuroxime acid of formula (III) with (R,S)-1-acetoxyethyl bromide of formula (IV), and a Group I or II metal carbonate in the presence of a compound of formula (V), MmHnPqOr  (V) wherein M is Group I or II metal; m is 1, 2, 3; n is 0, 1, 2, or 4; q is 1 or 2; r is 4, 7 or 8; in the presence of a C1-4 alcohol and a polar tertiary amide solvent selected from N,N-dimethylacetamide, N,N-dimethylformamide, N,N-dimetheylpropionamide, N,N-diethylacetamide, N,N-diethylformamide and N,N-diethylpropionamide at a temperature ranging from about −30 to +30° C. and subjecting the product thus obtained to a desired step of purification.
    • 制备具有至少96%纯度且基本上不含式(II)的类似的三异构体和其它杂质的式(I)头孢呋辛酯的方法。 该方法包括使式(III)的头孢呋辛酸与式(IV)的(R,S)-1-乙酰氧基乙基溴和I或II族金属碳酸盐在式(Ⅴ)化合物存在下反应, in-line-formula description =“In-line Formulas”end =“lead”?> M&lt;&lt;&lt; n&gt;&lt;&lt;&lt; (V)<?in-line-formula description =“In-line Formulas”end =“tail”?>其中M是I或II族金属; m为1,2,3; n为0,1,2或4; q为1或2; r为4,7或8; 在C 1-4醇和极性叔胺溶剂的存在下,选自N,N-二甲基乙酰胺,N,N-二甲基甲酰胺,N,N-二甲酰基丙酰胺,N,N-二乙基乙酰胺,N ,N-二乙基甲酰胺和N,N-二乙基丙酰胺,温度范围为约-30至+ 30℃,并将所得产物经过所需的纯化步骤。