摘要 |
A process for preparation of cefuroxime axetil of formula (I) of at least 96% purity and substantially free of analogous Delta<SUP>2</SUP>-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), <?in-line-formulae description="In-line Formulae" end="lead"?>M<SUB>m</SUB>H<SUB>n</SUB>P<SUB>q</SUB>O<SUB>r</SUB> (V)<?in-line-formulae description="In-line Formulae" end="tail"?> 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 C<SUB>1-4 </SUB>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.
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