公开(公告)号：US20050124029A1

公开(公告)日：2005-06-09

申请号：US10499662

申请日：2002-12-18

申请人： Wynand Alkema ,  Harold Moody ,  Jan Van Der Laan ,  Theodorus Johannes Van Dooren ,  Wilhelmus Hubertus Boesten

发明人： Wynand Alkema ,  Harold Moody ,  Jan Van Der Laan ,  Theodorus Johannes Van Dooren ,  Wilhelmus Hubertus Boesten

IPC分类号： C12N1/21 ,  C12N9/84 ,  C12N15/55 ,  C12P35/04 ,  C07D501/14 ,  C12N9/10

CPC分类号： C12N9/84

摘要： The invention relates to mutated penicillin acylases having a high synthesis/hydrolysis ratio in comparison with wild-type penicillin acylases and at least 1% of the activity. The invention also relates to a process for the enzymatic preparation of a β-lactam antibiotic from a β-lactam nucleus and an activated side chain with the aid of mutated penicillin acylases.

摘要翻译： 本发明涉及与野生型青霉素酰基转移酶相比具有高合成/水解比的突变青霉素酰基转移酶和至少1％的活性。 本发明还涉及借助于突变的青霉素酰基转移酶从β-内酰胺核和活化的侧链酶制备β-内酰胺抗生素的方法。

公开(公告)号：US20060035321A1

公开(公告)日：2006-02-16

申请号：US10515800

申请日：2003-05-23

申请人： Wilhelmus Hubertus Boesten ,  Joannes Kierkels ,  Bernard Assema ,  Luis Fuiz Perez ,  Dolores Gonzalez Pacanowska ,  Jesus Gonzalez Lopez ,  Santiago De La Escal Era Hueso

发明人： Wilhelmus Hubertus Boesten ,  Joannes Kierkels ,  Bernard Assema ,  Luis Fuiz Perez ,  Dolores Gonzalez Pacanowska ,  Jesus Gonzalez Lopez ,  Santiago De La Escal Era Hueso

IPC分类号： C12P13/04 ,  C07H21/04 ,  C12P21/06 ,  C12N9/90

CPC分类号： C12N9/90 ,  C12P13/04 ,  C12P41/00

摘要： The invention relates to isolated polypeptides with hydantoin recemase activity, that do not suffer from substrate inhibition. Such polypeptides arc for instance isolated polypeptides with at least 87% idcntity with SEQ ID: NO. 2 or SEQ ED: NO. 4. The invention also relates to nucleic acid sequences encoding these polypeptides. The invention also relates to processes for the racemisation of enantiomerically enriched hydantoin compounds and to processes for the preparation of enantiomarically enriched I)-or I-α amino acids.

摘要翻译： 本发明涉及具有乙内酰脲接收活性的分离的多肽，其不受底物抑制。 这样的多肽例如是与SEQ ID NO：具有至少87％的亲和性的分离的多肽。 2或SEQ ED：NO。 本发明还涉及编码这些多肽的核酸序列。 本发明还涉及对映体富集的乙内酰脲化合物的外消旋化方法以及制备对映体富集的I-I-I-α氨基酸的方法。

公开(公告)号：US20060258733A1

公开(公告)日：2006-11-16

申请号：US10554294

申请日：2004-04-28

申请人： Daniel Mink ,  Wilhelmus Hubertus Boesten ,  Michael Wolberg ,  Natasch Sereinig

发明人： Daniel Mink ,  Wilhelmus Hubertus Boesten ,  Michael Wolberg ,  Natasch Sereinig

IPC分类号： A61K31/401 ,  C07D309/30 ,  C07D319/06

CPC分类号： C07D309/30

摘要： The invention relates to a process for the preparation of (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile from 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one, wherein X stands for a leaving group, by reacting 6-X-substituted-methyl-4-hydroxy-tetrahydro-pyran-2-one with a cyanide ion in water and by subsequent lowering of the pH to a pH between 0 and 5. (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable from (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile may suitably be used in the preparation of a pharmaceutical preparation, more in particular in the preparation of statins, more in particular in the preparation of Atorvastatine or a salt thereof, for instance its calcium salt. The invention also relates to (4-hydroxy-6-oxo-tetrahydro-pyran-2-yl)-acetonitrile and other compounds obtainable therefrom.

摘要翻译： 本发明涉及从6-X取代的甲基-4-羟基 - 四氢 - 吡喃-2-酮制备（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈的方法， 其中X代表离去基团，通过使6-X取代的甲基-4-羟基 - 四氢 - 吡喃-2-酮与氰化物离子在水中反应，随后将pH降低至0至5之间的pH。 （4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈和从（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈获得的其它化合物可适当地用于制备 药物制剂，更特别是制备他汀类药物，更特别是制备阿托伐他汀或其盐，例如其钙盐。 本发明还涉及（4-羟基-6-氧代 - 四氢 - 吡喃-2-基） - 乙腈及其可得的其它化合物。