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PROCESS FOR THE PREPARATION OF CEPHRADINE

机译:头孢拉定的制备方法

摘要

The present invention describes a process for preparing cephradine, said process comprising reacting 7-aminodesacetoxy cephalosporanic acid (7-ADCA) with D-dihydrophenylglycine in activated form (DHa) in the presence of an enzyme in a reaction mixture to form cephradine, resulting in a conversion of 7-ADCA into cephradine of at least 70%, wherein the concentration D-dihydrophenylglycine (DH) in the reaction mixture is below 2 wt.%, wherein the conversion of 7-ADCA into cephradine & equals; (nCEF/n7-ADCA)*100%, wherein nCEF=quantity of cephradine formed (in mole); and n7-ADCA=total quantity of 7-ADCA added to reaction mixture (in mole). The invention also describes a process for the preparation of cephradine hydrate characterised in that the process comprises: -reacting 7-amino acid desacetoxy cephalosporanic acid (7-ADCA) with DHa in the presence of an enzyme in a reaction mixture to form cephradine; -preparing an aqueous solution comprising at least part of the cephradine; and crystallising the cephradine from said aqueous solution. The invention further describes cephradine hydrate obtainable by a process according to invention. The invention also describes cephradine hydrate with an absorbance at 450 nm of below 0.050.
机译:本发明描述了制备头孢拉定的方法,所述方法包括在反应混合物中在酶的存在下使7-氨基去乙酰氧基头孢菌酸(7-ADCA)与活化形式(DHa)的D-二氢苯基甘氨酸反应以形成头孢拉定。 7-ADCA到头孢拉定的转化率至少为70%,其中反应混合物中D-二氢苯基甘氨酸(DH)的浓度低于2重量%,其中7-ADCA到头孢拉定的转化率&等于; (nCEF / n7-ADCA)* 100%,其中nCEF =所形成的头孢拉定的量(以摩尔计); n7-ADCA =添加到反应混合物中的7-ADCA的总量(摩尔)。本发明还描述了制备头孢拉定水合物的方法,其特征在于该方法包括:-在反应混合物中,在酶的存在下,用DHa与DHA反应7-氨基酸的脱乙酰氧基头孢烷酸(7-ADCA)以形成头孢拉定。 -制备包含至少一部分头孢拉定的水溶液;从所述水溶液中结晶头孢拉定。本发明进一步描述了可通过根据本发明的方法获得的头孢拉定水合物。本发明还描述了头孢拉定水合物,其在450nm下的吸光度低于0.050。

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