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69 条记录 (耗时 0.031 秒)

    Substituted acetoxyazetidinone derivatives and process for preparing 4-acyloxyazetidinone derivatives
    31.
    发明授权
    Substituted acetoxyazetidinone derivatives and process for preparing 4-acyloxyazetidinone derivatives 失效
    取代的乙酰氧基氮杂环丁酮衍生物和制备4-酰氧基氮杂环丁酮衍生物的方法

    公开(公告)号：US5606052A

    公开(公告)日：1997-02-25

    申请号：US436812

    申请日：1995-05-08

    申请人： Takao Saito ,  Hidenori Kumobayashi ,  Shunichi Murahashi

    发明人： Takao Saito ,  Hidenori Kumobayashi ,  Shunichi Murahashi

    IPC分类号： B01J27/128 ,  B01J31/12 ,  B01J31/30 ,  C07B61/00 ,  C07D205/08 ,  C07F7/18

    CPC分类号： C07F7/186 ,  C07D205/08 ,  C07F7/1892

    摘要： A process for preparing a 4-acyloxyazetidinone or a derivative thereof represented by formula (IV): ##STR1## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a hydroxyethyl group, or a protected hydroxyethyl group; R.sup.3 represents an alkyl group having from 1 to 10 carbon atoms which may be substituted with a halogen atom, a cyano group, a lower alkoxy group or a phenyl group, or a substituted or unsubstituted phenyl group, provided that the .alpha.-positioned carbon atom of said alkyl group should not have more than two halogen atoms; and R.sup.4 represents a hydrogen atom, a lower alkyl group, or a lower alkoxycarbonyl group, which is useful as an intermediate for penem antibiotics is disclosed, comprising reacting azetidinone or a derivative thereof represented by formula (II): ##STR2## wherein R.sup.1 is as defined above, and R.sup.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxycarbonyl group, or a carboxyl group, with a carboxylic acid represented by formula (III):R.sup.3 COOH (III)wherein R.sup.3 is as defined above, in the presence of (1) a transition metal compound selected from a ruthenium compound, an osmium compound, and a cobalt compound, (2) an aldehyde having 2 or more carbon atoms, provided that the carbon atom at the .alpha.-position thereof should not have two or more halogen atoms, and (3) oxygen. The compound (IV) can be prepared with safety through simple and easy operations.

    摘要翻译： 制备由式（Ⅳ）表示的4-酰氧基氮杂环丁酮或其衍生物的方法：原子，低级烷基，羟乙基或被保护的羟乙基; R3表示可以被卤素原子，氰基，低级烷氧基或苯基取代的具有1至10个碳原子的烷基或取代或未取代的苯基，条件是α-位置的碳原子 的所述烷基不应具有多于两个的卤素原子; 其中R 4表示可用作Penem抗生素中间体的氢原子，低级烷基或低级烷氧基羰基，包括使由式（II）表示的氮杂环丁酮或其衍生物： 其中R 1如上所定义，R 2表示氢原子，低级烷基，低级烷氧基羰基或羧基，与式（III）表示的羧酸：R3COOH（III）其中R3如上定义 在（1）选自钌化合物，锇化合物和钴化合物的过渡金属化合物的存在下，（2）具有2个或更多个碳原子的醛，条件是其α位上的碳原子 不应该有两个或更多的卤素原子，和（3）氧。 化合物（IV）可以通过简单和容易的操作安全地制备。

    T-butyl (R)-(-)-4-cyano-3-hydroxybutyrate and process for preparing the same
    36.
    发明授权
    T-butyl (R)-(-)-4-cyano-3-hydroxybutyrate and process for preparing the same 失效
    （R） - （ - ） - 4-氰基-3-羟基丁酸叔丁酯及其制备方法

    公开(公告)号：US5430171A

    公开(公告)日：1995-07-04

    申请号：US272623

    申请日：1994-07-11

    申请人： Shigeru Mitsuhashi ,  Kazutoshi Sakurai ,  Hidenori Kumobayashi

    发明人： Shigeru Mitsuhashi ,  Kazutoshi Sakurai ,  Hidenori Kumobayashi

    IPC分类号： C07C253/14 ,  C07C255/20 ,  C07C255/23 ,  C07C255/12

    CPC分类号： C07C255/23

    摘要： T-butyl (R)-(-)-4-cyano-3-hydroxybutyrate having an optical purity of 99%ee or higher and a process for producing the same are disclosed, the process comprising cyanogenation of a t-butyl (S)-(-)-4-halogeno-3-hydroxybutyrate obtained by enantioselective hydrogenation of a t-butyl 4-halogenoacetoacetate. Recrystallization of the resulting crude product gives the optically active compound with high optical purity.

    摘要翻译： 公开了光学纯度为99％ee以上的（R） - （ - ） - 4-氰基-3-羟基丁酸叔丁酯及其制备方法，该方法包括将（S） - （ - ） - 4-卤代-3-羟基丁酸酯，通过4-卤代乙酰乙酸叔丁酯的对映选择性氢化得到。 所得粗产物的重结晶得到具有高光学纯度的光学活性化合物。

    (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative and production method thereof
    37.
    发明授权
    (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative and production method thereof 失效
    （3R，5S）-3,5,6-三羟基己酸衍生物及其制备方法

    公开(公告)号：US5286883A

    公开(公告)日：1994-02-15

    申请号：US976498

    申请日：1992-11-13

    申请人： Kazutoshi Sakurai ,  Shigeru Mitsuhashi ,  Hidenori Kumobayashi

    发明人： Kazutoshi Sakurai ,  Shigeru Mitsuhashi ,  Hidenori Kumobayashi

    IPC分类号： B01J31/24 ,  C07B53/00 ,  C07B61/00 ,  C07D309/12 ,  C07D319/06

    CPC分类号： C07D319/06 ,  C07D309/12

    摘要： A (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative and a process of producing the (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative which comprises the step of enantioselectively hydrogenating an (S)-5,6-dihydroxy-3-oxohexanoic acid derivative with a specific ruthenium-optically active phosphine complex represented as a catalyst are disclosed. The (3R,5S)-3,5,6-trihydroxyhexanoic acid derivative which is a useful compound capable of being easily converted into a lactone moiety, which is the active part of an inhibitor on HMG-CoA reductase, can be easily and efficiently obtained under a mild reaction condition with a high selectivity for the syn-diol form.

    摘要翻译： A（3R，5S）-3,5,6-三羟基己酸衍生物和（3R，5S）-3,5,6-三羟基己酸衍生物的制备方法，其包括以下步骤：对（S）-5 公开了以表示为催化剂的特定钌光学活性膦配合物的6-二羟基-3-氧代己酸衍生物。 作为HMG-CoA还原酶抑制剂的活性成分的能够容易地转化为内酯部分的有用化合物的（3R，5S）-3,5,6-三羟基己酸衍生物可以容易且有效地 在温和的反应条件下以对顺式二醇形式的高选择性获得。

    Process for preparing optically active 3-hydroxypyrrolidine derivatives
    39.
    发明授权
    Process for preparing optically active 3-hydroxypyrrolidine derivatives 失效
    制备光学活性3-羟基吡咯烷衍生物的方法

    公开(公告)号：US5144042A

    公开(公告)日：1992-09-01

    申请号：US682273

    申请日：1991-04-09

    申请人： Nobuo Seido ,  Yoshiki Okeda ,  Hidenori Kumobayashi

    发明人： Nobuo Seido ,  Yoshiki Okeda ,  Hidenori Kumobayashi

    IPC分类号： C07B53/00 ,  C07C31/34 ,  C07C211/27 ,  C07C309/65 ,  C07C309/73 ,  C07D207/12

    CPC分类号： C07D207/12

    摘要： A process for preparing optically active 3-hydroxypyrrolidine derivatives useful as intermediates represented by formula (III): ##STR1## wherein Q represents a substituted or unsubstituted phenyl group; and * indicates an asymmetric carbon atom, comprising reacting an optically active 4-halo-3-hydroxybutane derivative represented by formula (I): ##STR2## wherein * is as defined above; R.sup.1 represents a lower alkyl group or a substituted or unsubstituted phenyl group; and X represents a halogen atom, with a benzylamine derivative represented by formula (II):H.sub.2 NCH.sub.2 Q (II)wherein Q is as defined above, is disclosed. The starting compound (I) is easily available through chemical synthesis. Any complicated procedure or use of an expensive reagent is not required.