Process for preparing optically active oxazolidinone derivative
    1.
    发明授权
    Process for preparing optically active oxazolidinone derivative 失效
    光学活性恶唑烷酮衍生物的制备方法

    公开(公告)号:US06403804B1

    公开(公告)日:2002-06-11

    申请号:US09456950

    申请日:1999-12-07

    IPC分类号: C07D26304

    摘要: Disclosed is a process for preparing an optically active oxazolidinone derivative comprising allowing hydrazine to react on an optically active ester having a hydroxyl group at the 3-position which is represented by formula (II): wherein R1 represents a lower alkyl group having 1 to 4 carbon atoms, a phenyl group, a methoxymethyl group, a benzyloxymethyl group, a benzyloxycarbonylaminomethyl group which may have a substituent or substituents on the benzene ring thereof, an acylaminomethyl group having 3 to 10 carbon atoms, or an alkyloxycarbonylaminomethyl group having 3 to 6 carbon atoms; R2 and R3, which may be the same or different, each represent a hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a phenyl group, an acetylaminomethyl group, a benzoylaminomethyl group, or a benzyl group; and * indicates an asymmetric carbon atom, and subjecting the resulting hydrazide to Curtius rearrangement.

    摘要翻译: 公开了一种制备光学活性恶唑烷酮衍生物的方法,其包括使肼在由式(II)表示的3-位具有羟基的光学活性酯上反应:其中R1表示具有1-4个碳原子的低级烷基 碳原子,苯基,甲氧基甲基,苄氧基甲基,苯环上可以具有取代基的苄氧羰基氨基甲基,碳原子数3〜10的酰氨基甲基或碳原子数3〜6的烷氧基羰基氨基甲基 原子 R 2和R 3可以相同或不同,分别表示氢原子,碳原子数1〜4的低级烷基,苯基,乙酰氨基甲基,苯甲酰基氨基甲基或苄基。 和*表示不对称碳原子,并将所得酰肼进行柯氏重排。

    Process for preparing optically active 4-hydroxy-2-pyrrolidone
    5.
    发明授权
    Process for preparing optically active 4-hydroxy-2-pyrrolidone 失效
    制备光学活性4-羟基-2-吡咯烷酮的方法

    公开(公告)号:US5837877A

    公开(公告)日:1998-11-17

    申请号:US790931

    申请日:1997-01-29

    CPC分类号: C07D207/273

    摘要: A process for preparing optically active 4-hydroxy-2-pyrrolidone comprising asymmetrically hydrogenating an N-substituted-4-amino-3-oxobutanoic ester represented by formula (I): ##STR1## wherein R.sup.1 represents a benzyloxycarbonyl group, the benzene ring of which may be substituted; and R.sup.2 represents a lower alkyl group having 1 to 4 carbon atoms, in the presence of a ruthenium-optically active phosphine complex as a catalyst to obtain an optically active N-substituted-4-amino-3-hydroxybutanoic ester, deblocking, and cyclizing the ester. A series of the reactions can be carried out in one pot. Optically active 4-hydroxy-2-pyrrolidone is obtained in high yield with high optical purity, and is useful in the synthesis of carbapenem antibiotics

    摘要翻译: 一种制备光学活性的4-羟基-2-吡咯烷酮的方法,包括用式(I)表示的N-取代-4-氨基-3-氧代丁酸酯不对称氢化:其中R1代表苄氧基羰基, 苯环可以被取代; 在钌光学活性膦配合物作为催化剂的存在下,R 2表示具有1〜4个碳原子的低级烷基,得到光学活性的N-取代-4-氨基-3-羟基丁酸酯,去封闭和环化 酯。 一系列反应可以在一锅中进行。 以高光学纯度获得光学活性的4-羟基-2-吡咯烷酮,可用于合成碳青霉烯类抗生素

    T-butyl (R)-(-)-4-cyano-3-hydroxybutyrate and process for preparing the
same
    7.
    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

    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
    8.
    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

    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 producing optically active .gamma.-hydroxyketones
    9.
    发明授权
    Process for producing optically active .gamma.-hydroxyketones 失效
    光学活性γ-羟基酮的制备方法

    公开(公告)号:US5349107A

    公开(公告)日:1994-09-20

    申请号:US130173

    申请日:1993-10-01

    摘要: Disclosed herein is a process for producing a .gamma.-hydroxyketone (2), which comprises asymmetrically hydrogenating a .gamma.-diketone (1) in the presence of a ruthenium-optically active phosphine complex as a catalyst ##STR1## wherein R.sup.1 and R.sup.2 mean individually an alkyl or phenyl group which may have a substituent group. According to the invention, optically active .gamma.-hydroxyketones useful in synthesizing optically active moiety in, biodegradable polymers, perfumes, intermediates for synthesizing medicines and the like can be efficiently prepared.

    摘要翻译: 本文公开了一种制备γ-羟基酮(2)的方法,其包括在作为催化剂的钌光学活性膦配合物存在下不对称氢化γ-二酮(1),其中R 1和R 2分别表示 可以具有取代基的烷基或苯基。 根据本发明,可以有效地制备可用于合成光学活性部分的光学活性γ-羟基酮,可生物降解的聚合物,香料,用于合成药物的中间体等。