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    NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES
    2.
    发明申请
    NOVEL MANUFACTURING PROCESS FOR TRIAZINE, PYRIMIDINE AND PYRIDINE DERIVATIVES 审中-公开
    吡啶，吡嗪和吡啶衍生物的新型制备方法

    公开(公告)号：US20170037027A1

    公开(公告)日：2017-02-09

    申请号：US15304595

    申请日：2015-04-20

    申请人： UNIVERSITAET BASEL ,  PIQUR THERAPEUTICS AG

    发明人： Paul Hebeisen ,  Florent Beaufils ,  Jean-Baptiste Langlois

    IPC分类号： C07D401/04

    CPC分类号： C07D401/04 ,  A61K31/5377 ,  C07D213/127 ,  C07D213/53 ,  C07F5/025

    摘要： The invention relates to a method of manufacturing triazine, pyrimidine and pyridine derivatives of formula (I), wherein U, V, W and Z are nitrogen or carbon atoms, whereby at least one of U, V and W is nitrogen, and the other substituents are defined as in the specification, by condensing a corresponding halo-triazine, pyrimidine or pyridine in a type of Suzuki coupling with a pyridyl- or pyrimidinyl-borane, wherein the amino function is protected as a formamidine. The invention further relates to suitable intermediates and methods of manufacturing of such intermediates. Furthermore the invention relates to pure 5-(4,6-dimorpholino-1,3,5-triazin-2-yl)-4-(trifluoromethyl)pyridin-2-amine in solid form.

    摘要翻译： 本发明涉及一种制备式（I）的三嗪，嘧啶和吡啶衍生物的方法，其中U，V，W和Z是氮或碳原子，其中U，V和W中的至少一个是氮，而另一个 取代基如本说明书所定义，通过将一种类型的Suzuki偶联中的相应的卤代 - 三嗪，嘧啶或吡啶与吡啶基或嘧啶基 - 硼烷缩合，其中氨基官能团被保护为甲脒。 本发明进一步涉及合适的中间体及其制备方法。 此外，本发明涉及固体形式的纯的5-（4,6-二吗啉代-1,3,5-三嗪-2-基）-4-（三氟甲基）吡啶-2-胺。

    Organic compounds
    3.
    发明授权
    Organic compounds 有权
    有机化合物

    公开(公告)号：US08865905B2

    公开(公告)日：2014-10-21

    申请号：US13848178

    申请日：2013-03-21

    申请人： General Electric Company

    发明人： Yangang Liang ,  Shengxia Liu ,  Rui Wang ,  Jie Liu ,  Kelly Scott Chichak

    IPC分类号： C07D213/127 ,  C07D213/30 ,  H01L51/00 ,  C07D213/26

    CPC分类号： H01L51/0067 ,  C07D213/127 ,  C07D213/26 ,  C07D213/30

    摘要： A compound of formula IV: wherein R1, R2, and R3 are, independently at each occurrence, a C1-C20 aliphatic radical, a C3-C20 aromatic radical, or a C3-C20 cycloaliphatic radical; Ar is heteroaryl, aryl, alkyl or cycloalkyl; b and c are, independently at each occurrence, an integer ranging from 0-4; a is an integer ranging from 0-3; and n is an integer ranging from 2 to 4.

    摘要翻译： 式IV化合物：其中R 1，R 2和R 3在每次出现时独立地为C 1 -C 20脂族基团，C 3 -C 20芳族基团或C 3 -C 20脂环族基团; Ar是杂芳基，芳基，烷基或环烷基; b和c各自独立地为0-4的整数; a是0-3的整数; n为2〜4的整数。

    PROCESS FOR MAKING ORGANIC COMPOUNDS AND THE ORGANIC COMPOUNDS MADE THEREFROM
    6.
    发明申请
    PROCESS FOR MAKING ORGANIC COMPOUNDS AND THE ORGANIC COMPOUNDS MADE THEREFROM 有权
    制造有机化合物和有机化合物的方法

    公开(公告)号：US20120178938A1

    公开(公告)日：2012-07-12

    申请号：US13424531

    申请日：2012-03-20

    申请人： Yangang Liang ,  Shengxia Liu ,  Rui Wang ,  Jie Liu ,  Kelly Scott Chichak

    发明人： Yangang Liang ,  Shengxia Liu ,  Rui Wang ,  Jie Liu ,  Kelly Scott Chichak

    IPC分类号： C07D401/14

    CPC分类号： H01L51/0067 ,  C07D213/127 ,  C07D213/26 ,  C07D213/30

    摘要： A compound of formula II is prepared by: reacting a compound of formula F with 1-chloro-3,5-dibromobenzene to form a compound of formula G; reacting the compound of formula C with pinacol diborane to form a compound of formula H; reacting the compound of formula H with 1-bromo-3-iodobenzene to form a compound of formula J; and reacting the compound of formula J with pinacol diborane to form a compound of formula K; and reacting the compound of formula K with 3,5-dibromopyridine to form the compound of formula II.

    摘要翻译： 式Ⅱ化合物是通过使式F化合物与1-氯-3,5-二溴苯反应形成式G化合物; 使式C的化合物与频哪醇乙硼烷反应以形成式H的化合物; 使式H化合物与1-溴-3-碘苯反应形成式J化合物; 并使式J化合物与频哪醇乙硼烷反应以形成式K的化合物; 并使式K化合物与3,5-二溴吡啶反应，形成式Ⅱ化合物。

    PROCESS FOR PRODUCTION OF BIS-QUATERNARY AMMONIUM SALT, AND NOVEL INTERMEDIATE
    7.
    发明申请
    PROCESS FOR PRODUCTION OF BIS-QUATERNARY AMMONIUM SALT, AND NOVEL INTERMEDIATE 有权
    生产第四季铵盐和新型中间体的方法

    公开(公告)号：US20120130107A1

    公开(公告)日：2012-05-24

    申请号：US13387887

    申请日：2010-08-05

    申请人： Kuniaki Okamoto ,  Tsutomu Watahiki ,  Motoshige Sumino

    发明人： Kuniaki Okamoto ,  Tsutomu Watahiki ,  Motoshige Sumino

    IPC分类号： C07C309/73 ,  C07C303/32

    CPC分类号： C07D213/127 ,  C07C309/73 ,  C07D213/06 ,  C07D233/64 ,  H01M10/052 ,  H01M10/0567

    摘要： Object To provide a method for producing a bis-quaternary ammonium salt efficiently and a novel synthetic intermediate thereof.Solution The present invention relates to a method for producing a bis-quaternary ammonium salt represented by a general formula [3] which comprises reacting a disulfonic acid ester represented by a general formula [1] (in the formula, definitions of two R1's and T are as described in claim 1) with a tertiary amine represented by a general formula [2] (in the formula, definitions of R3 to R5 are as described in claim 1), and a disulfonic acid ester represented by a general formula [1′] (in the formula, two R16's represent independently a halogen atom or a C1-C3 fluoroalkyl group, and two m's represent independently an integer of 1 to 5).

    摘要翻译： 本发明提供一种双季铵盐生产方法及其新型合成中间体。 溶液本发明涉及由通式[3]表示的双季铵盐的制备方法，其包括使由通式[1]表示的二磺酸酯（式中，R 2和R 2的定义相同） 如通式[2]所示的叔胺（在该式中，R3至R5的定义如权利要求1所述）和由通式[1'表示的二磺酸酯如通式 （式中，两个R 16独立地表示卤素原子或C1-C3氟代烷基，2m独立地表示1〜5的整数）。

    PROCESS FOR PREPARATION OF E-ISOMER OF 1-(4-METHYLPHENYL) - 1-(2-PYRID YL)-3-PYRROLIDINO PROP-1-ENE AND ACID ADDITION SALTS THEREOF
    10.
    发明申请
    PROCESS FOR PREPARATION OF E-ISOMER OF 1-(4-METHYLPHENYL) - 1-(2-PYRID YL)-3-PYRROLIDINO PROP-1-ENE AND ACID ADDITION SALTS THEREOF 有权
    1-（4-甲基苯基）-1-（2-吡啶基）-3-吡咯烷酮丙-1-酮及其酸加成盐的异构体的制备方法

    公开(公告)号：US20110046384A1

    公开(公告)日：2011-02-24

    申请号：US12808516

    申请日：2008-12-16

    申请人： Rajender Pershad Gupta ,  Veerabhadra Swamy Hiremath ,  Raghavendra Arekal Vasanna ,  Vasantha Gowda Nekkilar

    发明人： Rajender Pershad Gupta ,  Veerabhadra Swamy Hiremath ,  Raghavendra Arekal Vasanna ,  Vasantha Gowda Nekkilar

    IPC分类号： C07D401/06

    CPC分类号： C07D213/127

    摘要： A process for preparation of E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula-I, and acid addition salts thereof, said process comprising; dehydrating 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinopropan-1-ol of Formula III followed by adding a base solution to obtain a mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene, and washing said mixture of E and Z isomers of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene with water to dissolve Z isomer and to obtain E-isomer of 1-(4-methylphenyl)-1-(2-pyridyl)-3-pyrrolidinoprop-1-ene of Formula I, which is substantially free from Z isomer.

    摘要翻译： 制备式I的1-（4-甲基苯基）-1-（2-吡啶基）-3-吡咯烷丙-1-烯的E-异构体及其酸加成盐的方法，所述方法包括： 使式III的1-（4-甲基苯基）-1-（2-吡啶基）-3-吡咯烷丙-1-醇脱水，然后加入碱溶液，得到1-（4-甲基苯基） -1-（2-吡啶基）-3-吡咯烷丙-1-烯，并洗涤1-（4-甲基苯基）-1-（2-吡啶基）-3-吡咯烷丙-1-烯的E和Z异构体混合物 用水溶解Z异构体并得到基本上不含Z异构体的式I的1-（4-甲基苯基）-1-（2-吡啶基）-3-吡咯烷丙-1-烯的E-异构体。