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    Process for the Synthesis of Cefaclor
    1.
    发明申请
    Process for the Synthesis of Cefaclor 有权
    头孢克洛合成方法

    公开(公告)号：US20080050771A1

    公开(公告)日：2008-02-28

    申请号：US11794119

    申请日：2005-12-23

    申请人： Harold Moody ,  Theodorus Johannes Goldfried Maria Dooren

    发明人： Harold Moody ,  Theodorus Johannes Goldfried Maria Dooren

    IPC分类号： C12P35/00 ,  C07D501/02

    CPC分类号： C12P35/04 ,  C07D501/58 ,  C12P35/00

    摘要： The present invention relates to a process for the synthesis of cefaclor, which process comprises reacting 7-amino-3-chloro cephalosporanic acid (7-ACCA) with D-phenylglycine in activated form (PGa) in the presence of an enzyme in a reaction mixture to form cefaclor, wherein at least part of 7-ACCA and/or PGa are added to the reaction mixture during the course of the reaction. The invention also relates to an aqueous mixture comprising an amount of cefaclor of >10 (w/w) %, an amount of 7-amino-3-chloro cephalosporanic acid of

    摘要翻译： 本发明涉及一种头孢克洛的合成方法，该方法包括使7-氨基-3-氯头孢菌酸（7-ACCA）与活性形式的D-苯基甘氨酸（PGa）在酶的存在下反应 混合物以形成头孢克洛，其中在反应过程中将7-ACCA和/或PGa的至少一部分加入到反应混合物中。 本发明还涉及包含一定量的头孢克洛> 10（w / w）％，7-氨基-3-氯头孢菌酸的量<2（w / w）％和D量 （w / w）％的苯基甘氨酸和从该水性混合物中回收头孢克洛的方法。 本发明还涉及具有小于0.250的在400nm（A≤400）的吸光度的晶体形式的头孢克洛。

    Process for the preparation of cephradine
    4.
    发明申请
    Process for the preparation of cephradine 有权
    制备头孢拉定的方法

    公开(公告)号：US20060189802A1

    公开(公告)日：2006-08-24

    申请号：US10562345

    申请日：2004-07-01

    申请人： Dennis Heemskerk ,  Anja Gerarda Hogenboom ,  Carlos Lenhardt ,  Harold Moody ,  Theodorus Johannes Godfried Maria Dooren

    发明人： Dennis Heemskerk ,  Anja Gerarda Hogenboom ,  Carlos Lenhardt ,  Harold Moody ,  Theodorus Johannes Godfried Maria Dooren

    IPC分类号： C07D501/14

    CPC分类号： C07D501/00 ,  C12P35/04

    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.

    摘要翻译： 本发明描述了一种制备头孢拉定的方法，所述方法包括使7-氨基二乙酰氧基头孢菌酸（7-ADCA）与活化形式的二氢苯基甘氨酸（DHa）在酶的存在下在反应混合物中反应形成头孢拉定，得到 将7-ADCA转化为至少70％的头孢拉定，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转化成头孢拉定等于; （％CEF / n 7-ADCA）* 100％，其中n CEF =形成的头孢拉定量（以摩尔计）; 和n 7-ADCA =加入到反应混合物中的7-ADCA的总量（以摩尔计）。 本发明还描述了一种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7-氨基酸脱乙酰氧基头孢菌酸（7-ADCA）与DHa反应形成头孢拉定; - 制备包含至少一部分头孢拉定的水溶液; 并从所述水溶液中结晶头孢拉定。 本发明还描述了通过根据本发明的方法获得的头孢拉定水合物。 本发明还描述了在450nm处的吸光度低于0.050的头孢拉定水合物。