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208 条记录 (耗时 0.046 秒)

    Method for producing optically active naphthalene compound
    6.
    发明授权
    Method for producing optically active naphthalene compound 有权
    光学活性萘化合物的制造方法

    公开(公告)号：US09181217B2

    公开(公告)日：2015-11-10

    申请号：US14240466

    申请日：2012-08-24

    申请人： Koji Matsuyama ,  Masanori Hatsuda ,  Masahiko Yoshinaga ,  Mitsuhiro Yada ,  Koichi Tanimoto

    发明人： Koji Matsuyama ,  Masanori Hatsuda ,  Masahiko Yoshinaga ,  Mitsuhiro Yada ,  Koichi Tanimoto

    IPC分类号： C07B53/00 ,  C07C25/06 ,  C07C255/03 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07B53/00 ,  C07C25/06 ,  C07C255/03

    摘要： The present invention provides an industrially advantageous method for producing an optically active naphthalene compound useful as a therapeutic agent for dermatitis or the like. Specifically, the present invention provides a method for producing an optically active naphthalene compound [I], which comprises: a step of reacting a compound [a-1] and a compound [b-1] with each other in the presence of a base and a catalyst that is composed of a Pd compound and a tertiary phosphine ligand (step a); a step of asymmetrically hydrogenating a compound [c-1] in the presence of a hydrogen donor and a complex that is prepared from a ruthenium compound and a chiral ligand, or alternatively in the presence of an optically active oxazaborolidine compound (a CBS catalyst) and a boron hydride compound (step b); and a step of treating a compound [d-1] with a reducing agent (step c). (In the above formulae, Ra and Rb represent the same or different lower alkyl groups; and X1 represents a halogen atom.).

    摘要翻译： 本发明提供了用于制造用作皮炎等的治疗剂的光学活性萘化合物的工业上有利的方法。 具体而言，本发明提供了一种光学活性萘化合物[I]的制造方法，其特征在于，在碱的存在下，使化合物[a-1]和化合物[b-1] 和由Pd化合物和叔膦配体组成的催化剂（步骤a）; 在氢供体和由钌化合物和手性配体制备的络合物的存在下，或者在光学活性的恶唑硼烷化合物（CBS催化剂）存在下，不对称地氢化化合物[c-1] 和硼氢化合物（步骤b）; 和用还原剂处理化合物[d-1]（步骤c）的步骤。 （上述式中，Ra和Rb表示相同或不同的低级烷基，X1表示卤素原子。

    Succinic acid diester derivative, process for production thereof, and use of the derivative in the production of pharmaceutical preparation
    9.
    发明授权
    Succinic acid diester derivative, process for production thereof, and use of the derivative in the production of pharmaceutical preparation 有权
    琥珀酸二酯衍生物，其制备方法，以及衍生物在制备药物中的用途

    公开(公告)号：US08106230B2

    公开(公告)日：2012-01-31

    申请号：US12310524

    申请日：2007-08-30

    申请人： Takashi Inagaki ,  Yoshikazu Yamakawa

    发明人： Takashi Inagaki ,  Yoshikazu Yamakawa

    IPC分类号： C07C255/03 ,  C07C299/04

    CPC分类号： C07D207/416 ,  C07B53/00 ,  C07C269/06 ,  C07C271/22 ,  C07C2601/14

    摘要： The present invention provides with a process of preparing an optically active succinimide derivative, which is a key intermediate for production of ranirestat. A compound (3) is easily prepared by treating the derivative of succinic acid diester of the formula (2): wherein R1 is an amino group protected with a group removed by hydrogenolysis or a tert-butoxycarbonylamino group and R2 is an ethyl group optionally substituted with one or two methyl group(s) at α-position, provided that R2 is not a tert-butyl group when R1 is a tert-butoxycarbonylamino group; with alkali metal alkoxide and the compound (3) can be an important intermediate for production of ranirestat.

    摘要翻译： 本发明提供了制备光学活性琥珀酰亚胺衍生物的方法，该衍生物是生产ranirestat的关键中间体。 通过处理式（2）的琥珀酸二酯的衍生物容易地制备化合物（3）：其中R1是被氢解除去的基团保护的氨基或叔丁氧基羰基氨基，R2是任选取代的乙基 在α位具有一个或两个甲基，条件是当R 1是叔丁氧基羰基氨基时，R 2不是叔丁基; 与碱金属醇盐和化合物（3）可以作为生产ranirestat的重要中间体。