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    Catalytic preparation of optically active ketones
    1.
    发明公开
    Catalytic preparation of optically active ketones 失效
    凯蒂琳·赫斯特伦

    公开(公告)号：EP0409530A1

    公开(公告)日：1991-01-23

    申请号：EP90307750.1

    申请日：1990-07-16

    申请人： Takasago International Corporation

    发明人： Seido, Nobuo ,  Kumobayashi, Hidenori

    IPC分类号： C07C49/385 ,  C07C45/62

    CPC分类号： C07C49/395 ,  C07C45/62 ,  C07C49/403

    摘要： An α,β-unsaturated ketone of formula:
    wherein R¹ represents hydrogen or C1-5 alkyl (e.g. 2-ethyli­dene, 2-propylidene or 2-pentylidene cyclopentanone or 2-methylene cyclohexanone) is hydrogenated in an organic solvent at a hydrogen pressure of 10 to 150 kg/cm² at a temperature of 10 to 100°C for 10 to 150 hours with as catalyst a complex of an optically active phosphine with ruthenium; the solvent is removed and there is recovered as product the corresponding saturated ketone, of optical activity according to that of the catalyst.
    Suitable catalysts (see formulae (111) and (IV) contain a Ru halide complexed to the "BINAP" phosphine wherein the four phenyl groups may have para- methyl or t-butyl substituents.
    The ketone product is obtained in high purity and can be used for synthesis of prostaglandins or xanthine derivatives.

    摘要翻译： 其中R 1表示氢或C 1-5烷基（例如2-亚乙基，2-亚丙基或2-亚戊基环戊酮或2-亚甲基环己酮）的α，β-不饱和酮，其中R 1表示氢或有机 溶剂在10〜150kg / cm 2的氢气压力下，在10〜100℃的温度下进行10〜150小时，作为催化剂，光学活性膦与钌的络合物; 除去溶剂，作为产物回收相应的饱和酮，根据催化剂的光学活性。 合适的催化剂（参见式（111）和（IV））含有与“BINAP”膦络合的Ru卤化物，其中四个苯基可以具有对甲基或叔丁基取代基，得到高产纯度的酮产物， 用于合成前列腺素或黄嘌呤衍生物。

    2-Phenyl-2-(2'-piperidinylidene) acetate derivative, process for manufacturing the same, and process for manufacturing optically active 2-phenyl-2(2'-piperidinyl) acetate derivative by asymmetrically hydrogenating the same
    2.
    发明公开
    2-Phenyl-2-(2'-piperidinylidene) acetate derivative, process for manufacturing the same, and process for manufacturing optically active 2-phenyl-2(2'-piperidinyl) acetate derivative by asymmetrically hydrogenating the same 失效
    2-苯基-2-（2“哌啶基）乙酸酯衍生物，它们的制备方法，和通过不对称氢化光学活性的2-苯基-2-（2'-哌啶）乙酸乙酯衍生物的方法

    公开(公告)号：EP0860432A1

    公开(公告)日：1998-08-26

    申请号：EP98400387.1

    申请日：1998-02-18

    申请人： Takasago International Corporation

    发明人： Seido, Nobuo ,  Nishikawa, Takenobu ,  Sotoguchi, Tsukasa ,  Yuasa, Yoshifumi ,  Miura, Takashi ,  Kumobayashi, Hidenori

    IPC分类号： C07D211/70

    CPC分类号： C07C229/34 ,  C07C271/22 ,  C07D211/70

    摘要： Disclosed is a 2-phenyl-2-(2'-piperidinylidene)acetate derivative of formula(1) suitably used for a raw material of a 2-phenyl-2-(2'-piperidinyl)acetate derivative of formula(3)and a process for manufacturing the same. Also disclosed is a process for manufacturing an optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative which is a major intermediate for an antidepressant. The 2-phenyl-2-(2'-piperidinylidene)acetate derivative is manufactured by cyclizing a 7-(N-substituted amino)-3-oxo-2-heptanoate derivative of formula(2). The optically active 2-phenyl-2-(2'-piperidinyl)acetate derivative is manufactured by asymmetrically hydrogenating the 2-phenyl-2-(2'-piperidinylidene)acetate derivative in the presence of a complex of a Group VIII transition metal or an acid.

    摘要翻译： 公开的是2-苯基-2-（2'-哌啶基）的式乙酸酯衍生物（1）合适地用于原料的2-苯基-2-（2'-哌啶基）的式乙酸酯衍生物（3）和 用于制造它们的方法。 所以公开了一种用于制造光学活性的2-苯基-2-（2'-哌啶基）乙酸酯衍生物的方法，该方法是用于抗抑郁药的主要中间体。 2-苯基-2-（2'-哌啶基）乙酸酯衍生物是通过环化一个7-（N-取代的氨基）。制造式-3-氧代-2-庚衍生物（2）。 的光学活性的2-苯基-2-（2'-哌啶基）乙酸酯衍生物是通过不对称氢化的2-苯基-2-（2'-哌啶基）乙酸酯衍生物在第Ⅷ族过渡金属的复合物的存在或制造 上酸。

    A process for producing optically active pyrrolidine derivatives
    3.
    发明公开
    A process for producing optically active pyrrolidine derivatives 失效
    Verfahren zur Herstellung optisch aktiver吡咯烷

    公开(公告)号：EP0855390A1

    公开(公告)日：1998-07-29

    申请号：EP98400146.1

    申请日：1998-01-23

    申请人： Takasago International Corporation

    发明人： Yuwasa, Yosifumi ,  Sotoguchi, Tsukasa ,  Seido, Nobuo

    IPC分类号： C07D207/08 ,  C07D207/09

    CPC分类号： C07D207/08 ,  C07D207/09 ,  C07D207/26

    摘要： An optically active (3R,1'S)-3-[(1'-N-methylamino)ethyl]pyrrolidine is used as an intermediate for synthesis of pharmaceutical preparations such as anti-fungus agents. This product can be obtained in a new process having fewer steps, with higher purity and in higher yield, than in conventional processes. This new process comprises subjecting 3-acetyl-1-benzyl-2-pyrrolidinone to asymmetric hydrogenation by use of a complex formed from bidentate phosphine and ruthenium as a catalyst to produce (3S,1'R)-1-benzyl-3-[(1'-hydroxy)ethyl]-2-pyrrolidinone, then reducing it with a hydride to give (3R,1'R)-1-benzyl-3-[(1'-hydroxy)ethyl]pyrrolidine, mesylating or tosylating it to give (3R,1'R)-1-benzyl-3-[(1'-methanesulfonyloxy)ethyl]pyrrolidine or (3R,1'R)-1-benzyl-3-[(1'-p-toluenesulfonyloxy)ethyl]pyrrolidine, reacting it with methylamine, whereby (3R,1'S)-1-benzyl-3-[(1'-N-methylamino)ethyl]pyrrolidine (5) is obtained, and this product is subjected to de-benzylation so that (3R,1'S)-3-[(1'-N-methylamino)ethyl]pyrrolidine is produced.

    摘要翻译： 使用光学活性（3R，1'S）-3-Ä（1'-N-甲基氨基）乙基吡咯烷作为合成药物制剂如抗真菌剂的中间体。 该产品可以以比常规方法更少的步骤获得，具有更高纯度和更高收率的新方法。 该新方法包括使用由二齿膦和钌形成的络合物作为催化剂，使3-乙酰基-1-苄基-2-吡咯烷酮进行不对称氢化，得到（3S，1'R）-1-苄基-3- （1'-羟基）乙基-2H-吡咯烷酮，然后用氢化物还原，得到（3R，1'R）-1-苄基-3-（1'-羟基）乙基吡咯烷，甲磺酰化或甲苯磺酸化，得到 3R，1'R）-1-苄基-3-（1'-甲磺酰氧基）乙基吡咯烷或（3R，1'R）-1-苄基-3-（1'-对甲苯磺酰氧基）乙基吡咯烷，使其与 甲基胺，由此得到（3R，1'S）-1-苄基-3-（1'-N-甲基氨基）乙基吡咯烷（5），该产物进行脱苄基化，使得（3R，1'S）-3- 制备Ä（1'-N-甲基氨基）乙基吡咯烷。

    Process for preparing optically active 6-t-butoxy-3,5-dihydroxyhexanoic esters
    4.
    发明公开
    Process for preparing optically active 6-t-butoxy-3,5-dihydroxyhexanoic esters 失效
    制备光学活性6-T-BUTOXY-3,5-二羟基己酸酯的方法

    公开(公告)号：EP0385733A3

    公开(公告)日：1991-01-09

    申请号：EP90302091.5

    申请日：1990-02-27

    申请人： Takasago International Corporation

    发明人： Seido, Nobuo ,  Sayo, Noboru ,  Kumobayashi, Hidenori

    IPC分类号： C07C69/708 ,  C07C67/31 ,  C07C67/343

    CPC分类号： C07C67/31 ,  C07C69/708

    摘要： An optically active 6-t-butoxy-3,5-dihydroxyhexanoic ester represented by the formula:
    wherein t-Bu represents a t-butyl group; and R represents a (C1-4) alkyl group,
    is prepared by asymmetrically hydrogenating a 4-t-butoxy­acetoacetic ester in an alcohol as solvent in the presence of a ruthenium-optically active tertiary phosphine complex of specified formula to obtain an optically active 4-t-­butoxy-3-hydroxy-butanoic ester, reacting the ester in an alcohol as solvent with a lithium enolate of an acetic ester to obtain an optically active 6-t-butoxy-5-hydroxy-­3-oxohexanoic ester, and asymmetrically hydrogenating the resulting ester in the presence of a diruthenium-tetrachloro optically active phosphine complex of specified formula as a catalyst. The desired product can be obtained in good yield at high stereoselectivity and is useful as a precursor of a lactone moiety of compactin, mevinolin or analogues there­of.

    Process for preparing optically active 6-t-butoxy-3,5-dihydroxyhexanoic esters
    7.
    发明公开
    Process for preparing optically active 6-t-butoxy-3,5-dihydroxyhexanoic esters 失效
    Verfahren zur Herstellung von optisch aktiven Estern der 6-t-Butoxy-3,5-dihydroxyhexansäure。

    公开(公告)号：EP0385733A2

    公开(公告)日：1990-09-05

    申请号：EP90302091.5

    申请日：1990-02-27

    申请人： Takasago International Corporation

    发明人： Seido, Nobuo ,  Sayo, Noboru ,  Kumobayashi, Hidenori

    IPC分类号： C07C69/708 ,  C07C67/31 ,  C07C67/343

    CPC分类号： C07C67/31 ,  C07C69/708

    摘要： An optically active 6-t-butoxy-3,5-dihydroxyhexanoic ester represented by the formula:
    wherein t-Bu represents a t-butyl group; and R represents a (C1-4) alkyl group,
    is prepared by asymmetrically hydrogenating a 4-t-butoxy­acetoacetic ester in an alcohol as solvent in the presence of a ruthenium-optically active tertiary phosphine complex of specified formula to obtain an optically active 4-t-­butoxy-3-hydroxy-butanoic ester, reacting the ester in an alcohol as solvent with a lithium enolate of an acetic ester to obtain an optically active 6-t-butoxy-5-hydroxy-­3-oxohexanoic ester, and asymmetrically hydrogenating the resulting ester in the presence of a diruthenium-tetrachloro optically active phosphine complex of specified formula as a catalyst.
    The desired product can be obtained in good yield at high stereoselectivity and is useful as a precursor of a lactone moiety of compactin, mevinolin or analogues there­of.

    摘要翻译： 由下式表示的光学活性的6-叔丁氧基-3,5-二羟基己酸酯：其中t-Bu表示叔丁基; R表示（C 1-4）烷基，是通过在具有规定式的钌光学活性叔膦络合物的存在下，在醇中作为溶剂不对称氢化4-叔丁氧基乙酰乙酸而得到光学活性4 叔丁氧基-3-羟基 - 丁酸酯，使酯在醇中作为溶剂与乙酸酯的烯醇化锂反应，得到光学活性的6-叔丁氧基-5-羟基-3-氧代己酸酯，不对称地 在具有规定的式钌 - 四氯光学活性膦配合物作为催化剂的存在下氢化所得的酯。 可以以高立体选择性以良好的产率获得所需的产物，并且可用作致密蛋白，美维林或其类似物的内酯部分的前体。

    Process for the preparation of piperidinylidene derivatives
    9.
    发明公开
    Process for the preparation of piperidinylidene derivatives 失效
    Verfahren zur Herstellung von Piperidylidenderivate

    公开(公告)号：EP0949247A1

    公开(公告)日：1999-10-13

    申请号：EP98303335.8

    申请日：1998-04-29

    申请人： Takasago International Corporation

    发明人： Nishikawa, Takenobu ,  Seido, Nobuo

    IPC分类号： C07D211/70

    CPC分类号： C07D211/70

    摘要： Disclosed is a process for economic, safe and simple production of a 2-phenyl-2-(2'-piperidinylidene)acetate derivative at a reduced number of steps in a high yield, which comprises allowing 2,3,4,5-Tetrahydro-6-methoxypyridine and a benzyl cyanide derivative represented by the following general formula (2):
    wherein R 1 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom or an amino group, to undergo condensation reaction in the presence of an organic base such as 1,8-diazabicyclo[5.4.0]-7-undecene or a transition metal complex as a catalyst to produce a 2-phenyl-2-(2'-piperidinylidene)acetonitrile derivative represented by the following general formula (4):
    wherein R 1 is as defined above; and the wavy line indicates a geometrical isomer, and then reacting with an alcohol in the presence of hydrogen chloride.

    摘要翻译： 公开了以高产率以减少数量的步骤经济，安全和简单地生产2-苯基-2-（2'-亚哌啶基）乙酸酯衍生物的方法，其包括使2,3,4,5-四氢 -6-甲氧基吡啶和由以下通式（2）表示的苄基氰衍生物：其中R 1表示氢原子，低级烷基，低级烷氧基，卤素原子或氨基的 在有机碱例如1,8-二氮杂双环[5.4.0] -7-十一碳烯或过渡金属络合物作为催化剂存在下进行缩合反应，生成2-苯基-2-（2'-亚哌啶基）乙腈衍生物 由以下通式（4）表示：其中R 1如上所定义; 并且波浪线表示几何异构体，然后在氯化氢存在下与醇反应。