- Synthesis method of cefbuperazone
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The invention discloses a synthesis method of cefbuperazone. The synthesis method comprises the following steps: (1) synthesizing an intermediate I, (2) carrying out an acylation reaction process, (3)removing a protecting group, (4) purifying an intermediate III, and (5) carrying out alcoholysis and purification treatment. According to the synthesis method of cefbuperazone, through scientific rawmaterial selection and design of synthesis process conditions, triethylamine is adopted as an acid-binding agent, so that the reaction stability is effectively improved, and the generation of byproducts is reduced; the m-cresol is adopted to carry out the reaction of removing the diphenyl methyl protecting group, so that the quality and the yield of the product are effectively improved; the synthesis method is stable in reaction process, safe, controllable, good in product quality, high in yield and suitable for industrial mass production.
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- 7α-methoxycephalosporins and pharmaceutical composition comprising the same
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A 7α-methoxycephalosporin represented by the general formula and a salt thereof: STR1 wherein R1 represents a hydrogen atom or a carboxyl-protecting group; R2 represents an organic group linked to the carbon atoms through an oxygen or sulfur atom; R3 represents a lower alkyl group; n is 0, 1 or 2; A represents a hydrogen atom or a substituted or unsubstituted alkyl group; and B represents a substituted or unsubstituted alkyl group. These compounds have a broad antibacterial spectrum and high resistance to β-lactamase produced from bacteria, and are well absorbed in a living body.
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