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    Process for producing pyrrole compound
    2.
    发明授权
    Process for producing pyrrole compound 有权
    制备吡咯化合物的方法

    公开(公告)号：US08822694B2

    公开(公告)日：2014-09-02

    申请号：US13203441

    申请日：2010-02-24

    申请人： Tomomi Ikemoto ,  Misayo Sera ,  Naohiro Fukuda

    发明人： Tomomi Ikemoto ,  Misayo Sera ,  Naohiro Fukuda

    IPC分类号： C07D401/12

    CPC分类号： C07D207/337 ,  C07D207/30 ,  C07D207/333 ,  C07D207/34 ,  C07D207/36 ,  C07D207/48 ,  C07D401/12

    摘要： The present invention provides a production method of a sulfonylpyrrole compound useful as a pharmaceutical product, a production method of an intermediate used for the method, and a novel intermediate. The present invention relates to a method of producing sulfonylpyrrole compound (VIII), which includes reducing compound (III) and hydrolyzing the reduced product to give compound (IV), subjecting compound (IV) to a sulfonylation reaction to give compound (VI), and subjecting compound (VI) to an amination reaction.

    摘要翻译： 本发明提供了可用作药物的磺酰基吡咯化合物的制备方法，用于该方法的中间体的制备方法和新的中间体。 本发明涉及一种制备磺酰基吡咯化合物（Ⅷ）的方法，其包括还原化合物（III）并水解还原产物得到化合物（Ⅳ），使化合物（Ⅳ）进行磺酰化反应得到化合物（Ⅵ）， 并使化合物（VI）进行胺化反应。

    ALPHA-CARBOLINE DERIVATIVES AND METHODS FOR PREPARATION THEREOF
    4.
    发明申请
    ALPHA-CARBOLINE DERIVATIVES AND METHODS FOR PREPARATION THEREOF 审中-公开
    ALPHA-CARBOLINE衍生物及其制备方法

    公开(公告)号：US20090326229A1

    公开(公告)日：2009-12-31

    申请号：US12376068

    申请日：2007-08-02

    申请人： Masahiro Mizuno ,  Hideya Mizufune ,  Misayo Sera ,  Masahiro Mineno ,  Tsuyoshi Ueda

    发明人： Masahiro Mizuno ,  Hideya Mizufune ,  Misayo Sera ,  Masahiro Mineno ,  Tsuyoshi Ueda

    IPC分类号： C07D471/02 ,  C07D213/72

    CPC分类号： C07D471/04 ,  C07D213/74 ,  C07D213/75 ,  C07D405/12

    摘要： To provide methods for preparing alpha-carboline derivatives in few steps, as well as conveniently and industrially advantageously. A method for preparation of a compound represented by Formula (II) or a salt thereof, comprising subjecting a compound represented by Formula (I) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base; a method for preparation of a compound represented by Formula (IX) or a salt thereof, comprising subjecting a compound represented by Formula (VII) or a salt thereof to a ring closure reaction in the presence of a palladium catalyst, a ligand, and a base, and subsequently to an aromatization reaction; and methods for preparation of compounds represented by Formulae (XV), (XVII), and (XIX) or a salt thereof, comprising subjecting respective compounds represented by Formulae (II) and (IX) or a salt thereof to a reaction for introducing a leaving group when necessary, and subsequently to a coupling reaction: wherein the symbols respectively represent the same meaning as defined in the present specification.

    摘要翻译： 提供在几个步骤中以及方便和工业上有利地制备α-咔啉衍生物的方法。 一种制备由式（II）表示的化合物或其盐的方法，包括在钯催化剂，配体和配体存在下，将式（I）表示的化合物或其盐进行闭环反应 基础; 一种制备由式（Ⅸ）表示的化合物或其盐的方法，包括在钯催化剂，配体和配体存在下使式（Ⅶ）表示的化合物或其盐进行闭环反应 碱，然后进行芳构化反应; 以及由式（XV），（XVII）和（XIX）表示的化合物或其盐制备化合物或其盐的方法，包括使由式（Ⅱ）和（Ⅸ）表示的各种化合物或其盐进行引入 在必要时离去基团，随后进行偶联反应：其中符号分别表示与本说明书中定义的相同的含义。

    Process for preparing optically active 2,3-dihydrobenzofuran compounds
    5.
    发明授权
    Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
    光学活性2,3-二氢苯并呋喃化合物的制备方法

    公开(公告)号：US07420070B2

    公开(公告)日：2008-09-02

    申请号：US11054371

    申请日：2005-02-09

    申请人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

    发明人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

    IPC分类号： C07D405/00 ,  C07D307/00

    CPC分类号： C07D307/79 ,  C07B2200/07 ,  C07D405/04 ,  C07F9/65742

    摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

    摘要翻译： 一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物对其进行光学拆分的2,3-二氢苯并呋喃化合物或其盐进行光学拆分：其中R 1， SUP>和R 2各自为氢或任选取代的烃基; R 3是任选取代的芳族基团; 并且C是除了氨基之外还可以具有取代基的苯环]。 该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

    Highly Selective Novel Amidation Method
    6.
    发明申请
    Highly Selective Novel Amidation Method 审中-公开
    高选择性的新型酰胺化方法

    公开(公告)号：US20070238721A1

    公开(公告)日：2007-10-11

    申请号：US11628906

    申请日：2005-06-10

    申请人： Atsushi Inagaki ,  Misayo Sera

    发明人： Atsushi Inagaki ,  Misayo Sera

    IPC分类号： A61K31/553 ,  C07D498/00

    CPC分类号： C07D267/14 ,  C07D413/06

    摘要： The present invention provides an industrial production method with a short process having a high yield of an aliphatic cyclic carboxamide having carboxyl group, which comprises reacting functional group-selectively using an inexpensive condensing agent without protecting the carboxyl group by esterification, that is, reacting carboxylic acid anhydride obtained by reacting carboxylic acid and tertiary carboxylic acid halide with aliphatic cyclic secondary amine having carboxyl group.

    摘要翻译： 本发明提供了具有高产率的具有羧基的脂肪族环状羧酰胺的短工艺的工业生产方法，其包括使用廉价的缩合剂选择性地使官能团反应而不通过酯化保护羧基，即使羧基 通过羧酸和叔羧酸卤化物与具有羧基的脂族环状仲胺反应获得的酸酐。

    Process for preparing optically active 2,3-dihydrobenzofuran compounds
    7.
    发明授权
    Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
    光学活性2,3-二氢苯并呋喃化合物的制备方法

    公开(公告)号：US06878831B2

    公开(公告)日：2005-04-12

    申请号：US10451723

    申请日：2001-12-27

    申请人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

    发明人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

    IPC分类号： C07D307/79 ,  C07D405/04 ,  C07F9/6574 ,  C07D307/78

    CPC分类号： C07D307/79 ,  C07B2200/07 ,  C07D405/04 ,  C07F9/65742

    摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

    摘要翻译： 一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物使其由通式或其盐表示的2,3-二氢苯并呋喃化合物进行光学拆分：[其中R 1和R 2' 2>各自为氢或任选取代的烃基; R 3是任选取代的芳基; 并且C是除了氨基之外还可以具有取代基的苯环]。 该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。

    Process for preparing optically active 2,3-dihydrobenzofuran compounds
    10.
    发明申请
    Process for preparing optically active 2,3-dihydrobenzofuran compounds 失效
    光学活性2,3-二氢苯并呋喃化合物的制备方法

    公开(公告)号：US20050171184A1

    公开(公告)日：2005-08-04

    申请号：US11054371

    申请日：2005-02-09

    申请人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

    发明人： Isao Aoki ,  Mari Adachi ,  Hiroyuki Tawada ,  Makoto Yamashita ,  Misayo Sera

    IPC分类号： C07D307/79 ,  C07D405/04 ,  C07F9/6574 ,  A61K31/4035 ,  C07D45/02

    CPC分类号： C07D307/79 ,  C07B2200/07 ,  C07D405/04 ,  C07F9/65742

    摘要： A process for preparing optically active 2,3-dihydrobenzofuran compounds which comprises subjecting a 2,3-dihydrobenzofuran compound represented by the general formula or a salt thereof to optical resolution with an optically active acid compound: [wherein R1 and R2 are each hydrogen or an optionally substituted hydrocarbon group; R3 is an optionally substituted aromatic group; and C is a benzene ring which may further have a substituent in addition to the amino group]. The process enables industrially advantageous production of intermediates for the synthesis of optically active 2,3-dihydrobenzofuran compounds useful as preventive and/or therapeutic drugs for neurodegenerative diseases and so on.

    摘要翻译： 一种制备光学活性2,3-二氢苯并呋喃化合物的方法，其包括用光学活性酸化合物对其进行光学拆分的2,3-二氢苯并呋喃化合物或其盐进行光学拆分：其中R 1， SUP>和R 2各自为氢或任选取代的烃基; R 3是任选取代的芳族基团; 并且C是除了氨基之外还可以具有取代基的苯环]。 该方法可以在工业上有利地生产用于合成可用作神经变性疾病等的预防和/或治疗药物的光学活性2,3-二氢苯并呋喃化合物的中间体。