公开(公告)号：US20050287650A1

公开(公告)日：2005-12-29

申请号：US11206574

申请日：2005-08-17

申请人： Joannes Theodorus Kierkels ,  Daniel Mink ,  Sven Panke ,  Franciscus Marie Lommen ,  Dennis Heemskerk

发明人： Joannes Theodorus Kierkels ,  Daniel Mink ,  Sven Panke ,  Franciscus Marie Lommen ,  Dennis Heemskerk

IPC分类号： C12N1/21 ,  C12N9/88 ,  C12N15/60 ,  C12P19/02

CPC分类号： C12N9/88 ,  C12P19/02

摘要： The invention relates to a process for the preparation of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose from a substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one α-hydrogen atom and a substituted or unsubstituted aldehyde in the presence of an aldolase and water, the reaction between the substituted or unsubstituted carbonyl compound with at least 2 carbon atoms and at least one α-hydrogen atom and the substituted or unsubstituted aldehyde being carried out at a carbonyl concentration of at most 6 moles/l of reaction mixture and the final concentration of the 2,4-dideoxyhexose or the 2,4,6-trideoxyhexose being at least 2 mass % of the reaction mixture. The invention also relates to the use of a 2,4-dideoxyhexose or a 2,4,6-trideoxyhexose obtained by means of a process according to the invention in the preparation of a medicine, particularly in the preparation of a statine.

摘要翻译： 本发明涉及从具有至少2个碳原子和至少一个α-氢原子的取代或未取代的羰基化合物和取代或未取代的羰基化合物制备2,4-二脱氧己糖或2,4,6-三脱氧己糖的方法， 未取代的醛在醛缩酶和水的存在下，取代或未取代的羰基化合物与至少2个碳原子和至少一个α-氢原子之间的反应和取代或未取代的醛以最多的羰基浓度进行 6摩尔/升的反应混合物，2,4-二脱氧己糖或2,4,6-三脱氧己糖的最终浓度为反应混合物的至少2质量％。 本发明还涉及通过根据本发明的方法获得的2,4-二脱氧己糖或2,4,6-三脱氧己糖在制备药物中的用途，特别是在制备他汀类药物中的用途。

公开(公告)号：US07588913B2

公开(公告)日：2009-09-15

申请号：US10562345

申请日：2004-07-01

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

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

IPC分类号： C12P35/04 ,  C07D501/22

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; （nCEF / n7-ADCA）* 100％，其中nCEF =形成的头孢拉定量（以摩尔计）; 和n7-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。

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。