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12 条记录 (耗时 0.024 秒)

    Process for Production of Lasofoxifene or Analogue Thereof
    1.
    发明申请
    Process for Production of Lasofoxifene or Analogue Thereof 有权
    拉索昔芬或其类似物的生产工艺

    公开(公告)号：US20090012314A1

    公开(公告)日：2009-01-08

    申请号：US12162068

    申请日：2007-01-25

    申请人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    发明人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    IPC分类号： C07D207/04 ,  C07C43/20 ,  C07C41/01

    CPC分类号： C07C67/287 ,  C07C41/24 ,  C07C41/26 ,  C07C41/32 ,  C07C67/293 ,  C07C2602/10 ,  C07D295/084 ,  C07C69/63 ,  C07C69/24 ,  C07C43/23

    摘要： Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.

    摘要翻译： 本发明公开了一种生产拉索昔芬，nafoxidine或其类似物的新方法，其包括减少数量的反应步骤，具有高效率，并且实际上是有利的。 为了生产拉索昔芬或其类似物，使用由式（4）表示的化合物作为中间体。 由式（4）表示的化合物可以通过在一个步骤中进行三种成分的偶联而使用由式（1）至（3）表示的化合物作为起始化合物来制备。

    Process for production of lasofoxifene or analogue thereof
    2.
    发明授权
    Process for production of lasofoxifene or analogue thereof 有权
    雷诺昔芬或其类似物的生产方法

    公开(公告)号：US08193394B2

    公开(公告)日：2012-06-05

    申请号：US12162068

    申请日：2007-01-25

    申请人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    发明人： Isamu Shiina ,  Yoshiyuki Sano ,  Kenya Nakata

    IPC分类号： C07C33/02

    CPC分类号： C07C67/287 ,  C07C41/24 ,  C07C41/26 ,  C07C41/32 ,  C07C67/293 ,  C07C2602/10 ,  C07D295/084 ,  C07C69/63 ,  C07C69/24 ,  C07C43/23

    摘要： Disclosed is a novel process for production of lasofoxifene, nafoxidine or an analogue thereof, which comprises reduced number of reaction steps, has a high efficiency, and is practically advantageous. For the production of lasofoxifene or an analogue thereof, a compound represented by the formula (4) is used as an intermediate. The compound represented by the formula (4) can be produced using compounds represented by the formulae (1) to (3) as starting compounds by performing the coupling of the three components in one step.

    摘要翻译： 本发明公开了一种生产拉索昔芬，nafoxidine或其类似物的新方法，其包括减少数量的反应步骤，具有高效率，并且实际上是有利的。 为了生产拉索昔芬或其类似物，使用由式（4）表示的化合物作为中间体。 由式（4）表示的化合物可以通过在一个步骤中进行三种成分的偶联而使用由式（1）至（3）表示的化合物作为起始化合物来制备。

    Method for producing optically active 2-hydroxy ester and novel intermediate compound
    7.
    发明授权
    Method for producing optically active 2-hydroxy ester and novel intermediate compound 有权
    光学活性2-羟基酯和新型中间体化合物的制备方法

    公开(公告)号：US08552215B2

    公开(公告)日：2013-10-08

    申请号：US13255465

    申请日：2010-03-08

    申请人： Isamu Shiina ,  Kenya Nakata

    发明人： Isamu Shiina ,  Kenya Nakata

    IPC分类号： C07C69/013

    CPC分类号： C07B53/00 ,  C07B57/00 ,  C07B2200/07 ,  C07C67/08 ,  C07F7/1804 ,  C07C69/734

    摘要： Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.

    摘要翻译： 公开了一种光学活性2-羟基酯的制备方法，该方法包括选择性地酯化含有催化剂的溶剂中的外消旋2-羟基酯的一种对映异构体，所述催化剂如四聚甲基或苯并四唑，以及羧酸酐或羧酸酐， 羧酸。 特别是在溶剂含有羧酸酐但不含有羧酸的情况下，作为羧酸酐，使用在a位含有叔或季碳原子的羧酸酐。 另一方面，在溶剂含有羧酸酐和羧酸的情况下，作为羧酸，使用在a位具有叔或季碳原子的羧酸。

    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-HYDROXY ESTER AND NOVEL INTERMEDIATE COMPOUND
    8.
    发明申请
    METHOD FOR PRODUCING OPTICALLY ACTIVE 2-HYDROXY ESTER AND NOVEL INTERMEDIATE COMPOUND 有权
    用于生产光学活性2-羟基酯和新型中间体化合物的方法

    公开(公告)号：US20110319650A1

    公开(公告)日：2011-12-29

    申请号：US13255465

    申请日：2010-03-08

    申请人： Isamu Shiina ,  Kenya Nakata

    发明人： Isamu Shiina ,  Kenya Nakata

    IPC分类号： C07C69/76 ,  C07C69/00

    CPC分类号： C07B53/00 ,  C07B57/00 ,  C07B2200/07 ,  C07C67/08 ,  C07F7/1804 ,  C07C69/734

    摘要： Disclosed is a method for producing an optically active 2-hydroxy ester, comprising selectively esterifying one enantiomer of a racemic 2-hydroxy ester in a solvent containing a catalyst such as tetramisole or benzotetramisole, and a carboxylic acid anhydride, or a carboxylic acid anhydride and a carboxylic acid. In particular, in the case where the solvent contains a carboxylic acid anhydride, but does not contain a carboxylic acid, as the carboxylic acid anhydride, a carboxylic acid anhydride containing a tertiary or quaternary carbon atom in the a-position is used. On the other hand, in the case where the solvent contains a carboxylic acid anhydride and a carboxylic acid, as the carboxylic acid, a carboxylic acid containing a tertiary or quaternary carbon atom in the a-position is used.

    摘要翻译： 公开了一种光学活性2-羟基酯的制备方法，该方法包括选择性地酯化含有催化剂的溶剂中的外消旋2-羟基酯的一种对映异构体，所述催化剂如四聚甲基或苯并四唑，以及羧酸酐或羧酸酐， 羧酸。 特别是在溶剂含有羧酸酐但不含有羧酸的情况下，作为羧酸酐，使用在a位含有叔或季碳原子的羧酸酐。 另一方面，在溶剂含有羧酸酐和羧酸的情况下，作为羧酸，使用在a位具有叔或季碳原子的羧酸。

    NOVEL DIHYDRONAPHTHALENE COMPOUND AND USE THEREOF
    9.
    发明申请
    NOVEL DIHYDRONAPHTHALENE COMPOUND AND USE THEREOF 有权
    新型二氢萘酚化合物及其用途

    公开(公告)号：US20100249400A1

    公开(公告)日：2010-09-30

    申请号：US12675331

    申请日：2008-09-11

    申请人： Isamu Shiina

    发明人： Isamu Shiina

    IPC分类号： C07D403/12 ,  C07D413/12 ,  C07C211/09 ,  C07D401/12

    CPC分类号： C07D295/088 ,  C07C217/24 ,  C07C2602/10

    摘要： Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent. (In the formula, two —(CH2)l—N(R1) (R2) groups represent a same substituent; R1 and R2 each represents a hydrogen atom, or a same or different alkyl group; or alternatively, R1 and R2 may combine together to form a monocyclic heterocyclic ring with a nitrogen atom having them or additionally together with one or more atoms selected from an oxygen atom, a sulfur atom and a nitrogen atom; R3, R4 and R5 each represents one or more substituents selected from a hydrogen atom, an alkyl group, an acyl group, an alicyclic group, an aromatic group, a halogen atom, an acyloxy group, a cyano group and a nitro group; l represents an integer of 2-5; n represents an integer of 1-4; m represents an integer of 1-5; and q represents an integer of 1-3.)

    摘要翻译： 公开了下述式（I）表示的化合物，其具有与拉索昔芬和nafoxidine相比具有优异的生产效率的化学结构的二氢化合物。 该化合物可用作蛋白酶体抑制剂和/或抗肿瘤剂。 （式中，二 - （CH 2）1 -N（R 1）（R 2）基团表示相同的取代基; R 1和R 2各自表示氢原子或相同或不同的烷基;或者，R 1和R 2可以组合 一起形成具有氮原子的单环杂环，或者另外与一个或多个选自氧原子，硫原子和氮原子的原子一起形成; R3，R4和R5各自表示一个或多个选自氢的取代基 原子，烷基，酰基，脂环族基团，芳香族基团，卤素原子，酰氧基，氰基和硝基; l表示2-5的整数; n表示1- 4; m表示1-5的整数，q表示1-3的整数。）

    Pyridine oxide compound, and process for producing carboxylic acid derivative and optically active carboxylic acid derivative with the use of the same
    10.
    发明授权
    Pyridine oxide compound, and process for producing carboxylic acid derivative and optically active carboxylic acid derivative with the use of the same 有权
    吡啶氧化物化合物，以及使用它们的羧酸衍生物和光学活性羧酸衍生物的制造方法

    公开(公告)号：US08034947B2

    公开(公告)日：2011-10-11

    申请号：US11816562

    申请日：2006-02-17

    申请人： Isamu Shiina

    发明人： Isamu Shiina

    IPC分类号： C07D213/22

    CPC分类号： C07C231/02 ,  C07B53/00 ,  C07B2200/07 ,  C07C67/08 ,  C07D213/89 ,  C07C69/24 ,  C07C69/612 ,  C07C69/007 ,  C07C233/65 ,  C07C233/78

    摘要： The invention relates to a pyridine oxide compound represented by formula (I), an optically active compound thereof, a salt thereof and a hydrate thereof, and, in the presence of the compound as a catalyst, performing 1) a method for producing an ester compound or an amide compound from a carboxylic acid equivalent and an alcohol or an amine, 2) an asymmetric esterification reaction or 3) an asymmetric amidation reaction. In formula (I), each R1 may be the same as the other R1 or different and each R1 represents an alkyl group, an aromatic group, a heterocyclic group, a carboxyl group, an ester group, a cyano group, a halogen atom, an oxygen atom, a sulfur atom or a nitrogen atom; each R2 may be the same as the other R2 or different and each R2 represents a hydrogen atom, an alkyl group, an aromatic group, a heterocyclic group, a carboxyl group, an ester group, a cyano group, a halogen atom, an oxygen atom or the like, and R3 and R4 may be the same or different and R3 and R4 each represent a hydrogen atom, an alkyl group, an aromatic group, a heterocyclic group, a carboxyl group, an ester group, a cyano group, a halogen atom, an oxygen atom or the like.

    摘要翻译： 本发明涉及由式（I）表示的吡啶氧化物，其光学活性化合物，其盐及其水合物，在作为催化剂的化合物的存在下，进行1）酯的制备方法 化合物或来自羧酸当量和醇或胺的酰胺化合物，2）不对称酯化反应或3）不对称酰胺化反应。 式（I）中，R 1可以相同或不同，R 1表示烷基，芳基，杂环基，羧基，酯基，氰基，卤素原子， 氧原子，硫原子或氮原子; 每个R 2可以与其它R 2相同或不同，每个R 2表示氢原子，烷基，芳基，杂环基，羧基，酯基，氰基，卤原子，氧 原子等，R3和R4可以相同或不同，R3和R4各自表示氢原子，烷基，芳基，杂环基，羧基，酯基，氰基， 卤素原子，氧原子等。