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227 条记录 (耗时 0.028 秒)

    Substituted acetylpyridine derivatives and process for the preparation of intermediates for optically active &bgr;3 agonist by the use of the same
    5.
    发明授权
    Substituted acetylpyridine derivatives and process for the preparation of intermediates for optically active &bgr;3 agonist by the use of the same 失效
    取代的乙酰基吡啶衍生物及其制备用于光学活性β3激动剂的中间体的方法

    公开(公告)号：US06642387B2

    公开(公告)日：2003-11-04

    申请号：US10305105

    申请日：2002-11-27

    申请人： Susumu Amano ,  Naoaki Taoka ,  Masaru Mitsuda ,  Kenji Inoue

    发明人： Susumu Amano ,  Naoaki Taoka ,  Masaru Mitsuda ,  Kenji Inoue

    IPC分类号： C07D21346

    CPC分类号： C07D213/30 ,  C07D213/50 ,  C07D213/74 ,  C07D213/75 ,  C07D405/04

    摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethylpyridine derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16)

    摘要翻译： 目的是以安全，有效和工业上有利的方式从容易获得的原料生产光学活性β-3肾上腺素受体激动剂的中间体。 由通式（9）表示的取代的乙酰基吡啶衍生物通过对映选择性还原反应来制备由通式（10）表示的光学活性羟乙基吡啶衍生物（其中*表示不对称碳原子），并进一步衍生为中间体 的光学活性β-3肾上腺素受体激动剂，例如由通式（14）表示的光学活性二羟基乙基吡啶衍生物或由通式（16）表示的光学活性环氧乙烷衍生物，

    Process for producing simvastatin
    6.
    发明授权
    Process for producing simvastatin 有权
    辛伐他汀生产工艺

    公开(公告)号：US06331641B1

    公开(公告)日：2001-12-18

    申请号：US09601794

    申请日：2000-09-28

    申请人： Naoaki Taoka ,  Kenji Inoue

    发明人： Naoaki Taoka ,  Kenji Inoue

    IPC分类号： C07D30930

    CPC分类号： C07D319/06 ,  C07D309/30 ,  Y02P20/55

    摘要： This invention provides an easy and efficient process for producing a simvastatin of great use as an HMG-CoA reductase inhibitor, which comprises deacylation of lovastatin with an inorganic base and a secondary or tertiary alcohol and subjecting the resulting diol lactone to selective protection with a ketal or acetal protective group, acylation and deprotection-lactonization to give simvastatin.

    摘要翻译： 本发明提供了一种用于生产作为HMG-CoA还原酶抑制剂的伟大用途的辛伐他汀的简单和有效的方法，其包括用无机碱和仲或叔醇脱氢洛伐他汀，并使所得二醇内酯用缩酮进行选择性保护 或缩醛保护基，酰化和去保护 - 内酯化得到辛伐他汀。

    Substituted acetylpridine derivatives and process for the preparation of intermediates for optically active beta-3 agonist by the use of the same
    7.
    发明授权
    Substituted acetylpridine derivatives and process for the preparation of intermediates for optically active beta-3 agonist by the use of the same 失效
    取代的乙酰嘌呤衍生物和通过使用它们制备光学活性β-3激动剂的中间体的方法

    公开(公告)号：US06515134B1

    公开(公告)日：2003-02-04

    申请号：US09926021

    申请日：2001-11-07

    申请人： Susumu Amano ,  Naoaki Taoka ,  Masaru Mitsuda ,  Kenji Inoue

    发明人： Susumu Amano ,  Naoaki Taoka ,  Masaru Mitsuda ,  Kenji Inoue

    IPC分类号： C07D21326

    CPC分类号： C07D213/30 ,  C07D213/50 ,  C07D213/74 ,  C07D213/75 ,  C07D405/04

    摘要： It is an objective to produce intermediates of optically active beta-3 adrenaline receptor agonists from readily available raw materials in a safe, efficient and industrially advantageous manner. A substituted acetylpyridine derivative represented by the general formula (9) is reduced by enantioselective reduction to produce an optically active hydroxyethyl derivative represented by the general formula (10) (wherein * represents an asymmetric carbon atom), and it is further derivatized to an intermediate of an optically active beta-3 adrenaline receptor agonist, such as an optically active dihydroxyethylpyridine derivative represented by the general formula (14) or an optically active oxirane derivative represented by the general formula (16).

    摘要翻译： 目的是以安全，有效和工业上有利的方式从容易获得的原料生产光学活性β-3肾上腺素受体激动剂的中间体。 由通式（9）表示的取代的乙酰基吡啶衍生物通过对映选择性还原而被还原，以制备由通式（10）表示的光学活性羟乙基衍生物（其中*表示不对称碳原子），并进一步衍生为中间体 的光学活性β-3肾上腺素受体激动剂，例如由通式（14）表示的光学活性二羟基乙基吡啶衍生物或由通式（16）表示的光学活性环氧乙烷衍生物。

    Process for producing L-allysine acetals
    8.
    发明授权
    Process for producing L-allysine acetals 失效
    生产L-赖氨酸乙缩醛的方法

    公开(公告)号：US06174707B1

    公开(公告)日：2001-01-16

    申请号：US09202901

    申请日：1999-03-04

    申请人： Naoaki Taoka ,  Takehiko Matsumoto ,  Kenji Inoue

    发明人： Naoaki Taoka ,  Takehiko Matsumoto ,  Kenji Inoue

    IPC分类号： G01N3853

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

    摘要： The present invention has for its object to provide a method for producing an L-allysine acetal which involves a fewer steps and is efficient. This invention relates to method for producing an L-allysine acetal which comprises; converting a D,L-allysine acetal of the following general formula (1) (wherein R1 and R2 are the same or different, and each of them represents an alkyl group having 1 to 8 carbon atoms, or they combinedly form a ring and represent an alkylene group having 2 to 8 carbon atoms) to a mixture of a 2-oxo-6,6-dialkoxyhexanoic acid of the following general formula (2) (wherein R1 and R2 are as defined above) and an L-allysine acetal of the following general formula (3) (wherein R1 and R2 are as defined above) by reacting in the presence of an enzyme capable of stereoselective oxidative deamination of D-amino acids and; isolating said L-allysine acetal after said converting.

    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，该方法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，其包括：将D，L-烯丙基乙缩醛 的下述通式（1）（其中，R 1和R 2相同或不同，它们各自表示碳原子数1〜8的烷基，或者它们组合形成环，表示碳原子数2〜8的亚烷基 原子）与下述通式（2）的2-氧代-6,6-二烷氧基己酸（其中R 1和R 2如上定义）和下列通式（3）的L-烯丙基缩醛的混合物 其中R1和R2如上所定义）通过在能够进行D-氨基酸的立体选择性氧化脱氨作用的酶存在下反应;和在所述转化后分离所述L-赖氨酸缩醛。

    Process for the preparation of optically active 2-[6-hydroxymethyl)-1,3-dioxan-4yl]acetic acid derivatives
    10.
    发明授权
    Process for the preparation of optically active 2-[6-hydroxymethyl)-1,3-dioxan-4yl]acetic acid derivatives 有权
    制备光学活性2-Ä6-（羟甲基）-1,3-二恶烷-4-基乙酸衍生物的方法

    公开(公告)号：US06472544B1

    公开(公告)日：2002-10-29

    申请号：US09509998

    申请日：2000-08-16

    申请人： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    发明人： Noriyuki Kizaki ,  Yukio Yamada ,  Yoshihiko Yasohara ,  Akira Nishiyama ,  Makoto Miyazaki ,  Masaru Mitsuda ,  Takeshi Kondo ,  Noboru Ueyama ,  Kenji Inoue

    IPC分类号： C07D31906

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

    摘要： This invention provides a process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives, which are of value as intermediates of drugs, from inexpensive starting materials without using any special equipment such as that required for super-low temperature reactions. A process for producing optically active 2-[6-(hydroxymethyl)-1,3-dioxan-4-yl]acetic acid derivatives which comprises reacting an acetic acid derivative at a temperature of not less than −30° C. with an enolate prepared by permitting either a base or a metal having a valency of 0 to act on the derivative to produce a hydroxyoxohexanoic acid derivative, reducing this compound with the aid of a strain of microorganism to provide a halomethyldioxanylacetic acid derivative, treating this compound with an acetalizing agent in the presence of an acid catalyst to provide a halomethyldioxanylacetic acid derivative, reacted with an acyloxylating agent to provide a acyloxymethyldioxanylacetic acid derivative, and subjecting this compound to solvolysis in the presence of a base.

    摘要翻译： 本发明提供了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的2- [6-（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 例如超低温反应所需的方法。一种制备光学活性的2- [6-（羟甲基）-1,3-二恶烷-4-基]乙酸衍生物的方法，其包括在不是的温度下使乙酸衍生物反应 小于-30℃，通过使碱金属或化合价为0的金属作用于衍生物以制备羟基氧代己酸衍生物而制备的烯醇化物，借助于微生物菌株还原该化合物以提供 卤甲基二恶烷基乙酸衍生物，在酸催化剂存在下用缩醛化剂处理该化合物，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 在碱的存在下，将该化合物施用于溶剂分解。