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    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2- 6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL]ACETIC ACID DERIVATIVES
    4.
    发明公开
    PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE 2- 6-(HYDROXYMETHYL)-1,3-DIOXAN-4-YL]ACETIC ACID DERIVATIVES 有权
    VERFAHREN ZUR HERSTELLUNG OPTISCH AKTIVER 2- [6-（羟甲基）-1,3-二氧戊环-4-基] - 维生素D

    公开(公告)号：EP1024139A4

    公开(公告)日：2002-04-17

    申请号：EP99935066

    申请日：1999-08-05

    申请人： KANEKA CORP

    发明人： KIZAKI NORIYUKI ,  YAMADA YUKIO ,  YASOHARA YOSHIHIKO ,  NISHIYAMA AKIRA ,  MIYAZAKI MAKOTO ,  MITSUDA MASARU ,  KONDO TAKESHI ,  UEYAMA NOBORU ,  INOUE KENJI

    IPC分类号： C07C67/343 ,  C07C253/30 ,  C07C255/21 ,  C07D319/06 ,  C12P7/62 ,  C07C67/31

    CPC分类号： C07D319/06 ,  C07B2200/07 ,  C07C67/343 ,  C07C253/30 ,  C12P7/62 ,  C07C69/716 ,  C07C255/21

    摘要： A process for the preparation of optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which comprises subjecting an enolate prepared by reacting an acetate ester derivative with either a base or a zero-valent metal to reaction with a hydroxybutyric acid derivative at -30 °C or above to thereby obtain a hydroxyoxohexanoic acid derivative, reducing this hydroxyoxohexanoic acid derivative with a microorganism into a dihydroxyhexanoic acid derivative, treating this dihydroxyhexanoic acid derivative with an acetal-forming reactant in the presence of an acid to thereby obtain a halomethyldioxanylacetic acid derivative, acyloxylating this halomethyldioxanylacetic acid derivative with an acyloxylating agent into an acyloxymethyldioxanylacetic acid derivative, and subjecting this acyloxymethyldioxanylacetic acid derivative to solvolysis in the presence of a base.

    摘要翻译： 本发明提供了一种从廉价起始原料生产具有价值作为药物中间体的光学活性2-Ä6-（羟甲基）-1,3-二恶烷-4-基乙酸衍生物的方法，而不使用任何特殊设备，例如 超低温反应需要。 制备光学活性2-δ-（羟甲基）-1,3-二恶烷-4-基乙酸衍生物的方法，其包括使不饱和-30℃的乙酸衍生物与烯醇化物反应 通过使碱价或0价金属作用于衍生物以制备羟基己酸衍生物而制备，借助于微生物菌株将该化合物还原，得到卤代甲基二恶烷基乙酸衍生物，用缩醛化处理该化合物 在酸催化剂存在下反应，得到卤代甲基二恶烷基乙酸衍生物，与酰氧基化剂反应，得到酰氧基甲基二恶烷基乙酸衍生物，并在碱的存在下使其溶解。

    PROCESSES FOR PRODUCING AZETIDINE-2-CARBOXYLIC ACID AND INTERMEDIATES THEREOF
    5.
    发明公开
    PROCESSES FOR PRODUCING AZETIDINE-2-CARBOXYLIC ACID AND INTERMEDIATES THEREOF 失效
    用于生产氮杂环丁烷-2-羧酸和其中间体

    公开(公告)号：EP0992491A4

    公开(公告)日：2000-07-19

    申请号：EP98917669

    申请日：1998-04-24

    申请人： KANEKA CORP

    发明人： AWAJI HIROSHI ,  MATSUMOTO SHINGO ,  INOUE KENJI ,  MATSUO KAZUHIKO

    IPC分类号： C07D205/04

    CPC分类号： C07D205/04 ,  Y02P20/55

    摘要： Efficient and economical processes for producing azetidine-2-carboxylic acid and intermediates thereof on an industrial scale. Azetidine-2-carboxylic acid of structural formula (5) is produced by reducing a 4-oxo-2-azetidinecarboxylic acid derivative of general formula (1) to form azetidine-2-methanol of structural formula (2), treating this compound with an amino-protecting agent to form an N-protected azetidine-2-methanol of general formula (3), treating this compound with an oxidizing agent to form an N-protected azetidine-2-carboxylic acid of general formula (4), and removing the amino-protecting group.

    PROCESS FOR PRODUCING (R)-2-HYDROXY-1-PHENOXYPROPANE DERIVATIVE
    7.
    发明公开
    PROCESS FOR PRODUCING (R)-2-HYDROXY-1-PHENOXYPROPANE DERIVATIVE 审中-公开
    VERFAHREN ZUR HERSTELLUNG EINES（R）-2-羟基-1-苯氧基丙烯酸酯

    公开(公告)号：EP1055732A4

    公开(公告)日：2003-03-12

    申请号：EP99959901

    申请日：1999-12-20

    申请人： KANEKA CORP

    发明人： TAOKA NAOAKI ,  KIZAKI NORIYUKI ,  YASOHARA YOSHIHIKO ,  INOUE KENJI ,  HASEGAWA JUNZO

    IPC分类号： C12P7/22 ,  C12P41/00 ,  C12R1/72

    CPC分类号： C12P7/22 ,  C12P41/002

    摘要： To efficiently produce an (R)-2-hydroxy-1-phenoxypropane derivative which is useful as a drug intermediate at a high optical purity, a phenoxyacetone derivative is R-selectively reduced by using a carbonyl reductase originating in candida, or an optionally processed culture medium of a microorganism capable of producing the above enzyme.

    摘要翻译： 为了高效率地制造作为光学纯度高的药物中间体有用的（R）-2-羟基-1-苯氧基丙烷衍生物，使用来源于念珠菌的羰基还原酶或任选加工的苯氧基丙酮衍生物进行R选择性还原 能够产生上述酶的微生物的培养基。

    PROCESS FOR PRODUCING L-ALLYSINE ACETALS
    8.
    发明公开
    PROCESS FOR PRODUCING L-ALLYSINE ACETALS 失效
    Verfahren zur Herstellung von L-Allysin Acetalen

    公开(公告)号：EP0919630A4

    公开(公告)日：2002-08-28

    申请号：EP98917612

    申请日：1998-04-22

    申请人： KANEKA CORP

    发明人： TAOKA NAOAKI ,  MATSUMOTO TAKEHIKO ,  INOUE KENJI

    IPC分类号： C12P7/40 ,  C12P7/42 ,  C12P13/04 ,  C12P41/00

    CPC分类号： C12P7/40 ,  C12P13/04 ,  C12P41/006

    摘要： A process for efficiently producing L-allysine acetals in short steps, which comprises reacting a D,L-allysine acetal of general formula: (1) (wherein R and R are the same or different from each other and each represents an alkyl group of 1 to 8 carbon atoms, or R and R together form a ring to represent an alkylene group having 2 to 8 carbon atoms) in the presence of an enzyme having the activity for sterically selectively and oxidatively deaminating D-amino acids to convert the D,L-allysine acetal into a mixture of a 2-oxo-6,6-dialkoxyhexanoic acid of general formula (2) (wherein R and R are each as defined above) with an L-allysine acetal of general formula (3) (wherein R and R are each as defined above) and then recovering the L-allysine acetal.

    摘要翻译： 本发明的目的是提供一种生产L-赖氨酸缩醛的方法，其涉及较少的步骤并且是有效的。 本发明涉及L-赖氨酸缩醛的制备方法，该方法包括： 转化下列通式（1）的D，L-烯丙基缩醛（其中R 1和R 2相同或不同，并且各自表示具有1至8个碳原子的烷基，或它们 （2）的2-氧代-6,6-二烷氧基己酸的混合物（其中R 1和R 2分别独立地表示碳原子数为2〜8的亚烷基） 如上所定义）和下列通式（3）的L-烯丙基缩醛（其中R 1和R 2如上定义）通过在能够进行立体选择性氧化脱氨作用的酶的存在下反应 氨基酸和 在所述转化后分离所述L-赖氨酸缩醛。

    PROCESS FOR PRODUCING 6-CYANOMETHYL-1,3-DIOXANE-4-ACETIC ACID DERIVATIVES
    9.
    发明公开
    PROCESS FOR PRODUCING 6-CYANOMETHYL-1,3-DIOXANE-4-ACETIC ACID DERIVATIVES 有权
    VERFAHREN ZUR HERSTELLUNG VON VERIVATEN DER 6-CYANOMETHYL-1,3-DIOXAN-4-ESSIGSAÜRE

    公开(公告)号：EP1077212A4

    公开(公告)日：2001-11-21

    申请号：EP99917207

    申请日：1999-04-28

    申请人： KANEKA CORP

    发明人： MITSUDA MASARU ,  MIYAZAKI MAKOTO ,  INOUE KENJI

    IPC分类号： C07C253/14 ,  C07C255/20 ,  C07D319/06 ,  C07D319/04

    CPC分类号： C07D319/06 ,  C07C253/14 ,  C07C255/20

    摘要： A process whereby 6-cyanomethyl-1,3-dioxane-4-acetic acid derivatives, which are important intermediates of an HMG coenzyme A reductase atorvastatin, can be industrially, easily and efficiently produced. This process comprises starting with a 3,5-dihydroxy-6-halohexane derivative, treating it with a cyaniding agent to thereby substitute the halogen atom with the cyano group (i.e., a cyanation reaction) and forming an acetal of a diol by using an acetal-forming agent in the presence of an acid catalyst (i.e., an acetal-formation reaction).

    摘要翻译： 作为HMG辅酶A还原酶阿托伐他汀的重要中间体的6-氰基甲基-1,3-二恶烷-4-乙酸衍生物的工艺可以在工业上，容易和有效地生产。 该方法包括从3,5-二羟基-6-卤代己烷衍生物开始，用氰化剂处理它，从而用氰基取代卤素原子（即氰化反应），并通过使用一种二醇形成二醇的缩醛 在酸催化剂存在下缩醛形成剂（即缩醛形成反应）。