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    METHOD FOR PREPARING METHYL (Z)-3-[[4-[METHYL[2-(4-METHYL-1-PIPERAZINYL)ACETYL]AMINO]PHEHYL]AMINO]PHENYLMETHYLENE)-OXINDOLE-6-CARBOXYLATE (INTEDANIB, NINTEDANIB)
    81.
    发明申请
    METHOD FOR PREPARING METHYL (Z)-3-[[4-[METHYL[2-(4-METHYL-1-PIPERAZINYL)ACETYL]AMINO]PHEHYL]AMINO]PHENYLMETHYLENE)-OXINDOLE-6-CARBOXYLATE (INTEDANIB, NINTEDANIB) 审中-公开

    公开(公告)号：US20180215735A1

    公开(公告)日：2018-08-02

    申请号：US15748196

    申请日：2016-07-28

    申请人： Zentiva k.s.

    发明人： Ludek MECA

    IPC分类号： C07D403/12 ,  C07B43/04

    CPC分类号： C07D403/12 ,  C07B43/04 ,  C07D209/34

    摘要： The invention relates to a method of synthesizing methyl (Z)-3-[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl] amino]phenylmethylene)-oxindole-6-carboxylate of formula (1), known under the generic name of intedanib or nintedanib. The present method comprises a) a reaction of methyl oxindole-6-carboxylate with acetic anhydride at a temperature of 130-140° C., providing methyl 1-acetyl-oxindole-6-carboxylate; b) a reaction of methyl 1-acetyl-oxindole-6-carboxylate of with trimethyl orthobenzoate and acetic anhydride in the presence of toluene, providing methyl (E)-1-acetyl-3-(methoxyphenylmethylene)-oxindole-6-carboxylate; c) a reaction (E)-1-acetyl-3-(methoxyphenylmethylene)-oxindole-6-carboxylate with N-(4-aminophenyl)-N,4-di-methyl-1-piperazine acetamide and subsequently with an alkali hydroxide or alkali alkoxide in methanol or ethanol without isolation of the intermediate, providing methyl (Z)-3-[[4-[methyl[2-(4-methyl-1-piperazinyl)acetyl]amino]phenyl] amino]phenylmethylene)-oxindole-6-carboxylate, wherein the reaction is conducted at a temperature of 50 to 100° C. (1)

    IMPROVED PROCESS FOR THE REDUCTIVE AMINATION OF HALOGEN-CONTAINING SUBSTRATES
    84.
    发明申请
    IMPROVED PROCESS FOR THE REDUCTIVE AMINATION OF HALOGEN-CONTAINING SUBSTRATES 有权

    公开(公告)号：US20170320812A1

    公开(公告)日：2017-11-09

    申请号：US15523864

    申请日：2015-11-14

    申请人： Taminco BVBA

    发明人： Kristof Moonen ,  Kim Dumoleijn ,  Laura Prati ,  Alberto Villa

    IPC分类号： C07C209/26 ,  A01N37/42 ,  C07B43/04 ,  C07C249/04

    CPC分类号： C07C209/26 ,  A01N37/42 ,  C07B43/04 ,  C07C211/29 ,  C07C249/04

    摘要： Disclosed is a process for performing a reductive amination of a first functional group in an organic feed substrate, which feed substrate comprises at least one further functional group containing a halogen atom, wherein the halogen atom is selected from the list consisting of chlorine, bromine, iodine, and combinations thereof, in the presence of hydrogen and a heterogeneous catalyst comprising at least one metal from the list of Pd, Pt, Rh, Ir, and Ru, and in absence of any catalytic amount of any second metal from the list consisting of Ag, Ni, Co, Sn, Bi, Cu, Au, and combinations thereof. The process is preferably applied for the reductive amination of 2-chloro-benzaldehyde to form 2-chloro-benzyldimethylamine, as an intermediate in the production of active agrochemical compounds and microbicides of the methoximinophenylglyoxylic ester series.

    METHOD FOR PREPARING PALBOCICLIB
    86.
    发明申请
    METHOD FOR PREPARING PALBOCICLIB 有权

    公开(公告)号：US20170247379A1

    公开(公告)日：2017-08-31

    申请号：US15595167

    申请日：2017-05-15

    申请人： SUZHOU MIRACPHARMA TECHNOLOGY CO., LTD.

    发明人： Xuenong XU

    IPC分类号： C07D471/04 ,  A61K31/535 ,  C08K5/03 ,  C08K5/34 ,  C08K5/3432 ,  A61K31/5395 ,  C07B43/04

    CPC分类号： C07D471/04 ,  A61K31/535 ,  A61K31/5395 ,  C07B43/04 ,  C08K5/03 ,  C08K5/34 ,  C08K5/3432

    摘要： The invention discloses a method for preparing Palbociclib (I). The preparation method comprises the steps of: causing a ring-closing reaction of 2-acetyl-2-butenoic acid methyl ester and malononitrile to occur in an alkaline condition to generate 1,4,5,6-tetrahydro-2-methoxyl-4-methyl-5-acetyl-6-oxy-3-pyridine carbonitrile (II); causing a substitution reaction of the intermediate(II) and halogenated cyclopentane(III) to occur under the effect of acid binding agent to generate N-cyclopentyl-1,4,5,6-tetrahydro-2-methoxyl-4-methyl-5-acetyl-6-oxy-3-pyridinecarbonitrile (IV); causing a condensation reaction of the intermediate(IV) and N-[5-(1-piperazinyl)-2-pyridinyl]guanidine (V) to occur to generate 6-acetyl-8-cyclopentyl-5,8-dihydro-5-methyl-2-[[5-(1-piperazinyl)-2-pyridinyl]amino]-pyrido[2,3-d]pyrimidin-7(6H)-one (VI); and causing a dehydrogenation reaction of the intermediate(VI) and sodium selenate to occur to prepare Palbociclib(I).The preparation method has readily available raw materials and a simple process, is economical and environmentally friendly, and is suitable for industrial production.

    PROCESS FOR PRODUCING SUBSTITUTED METHYLAMINE COMPOUND AND TRIAZINE DERIVATIVE
    90.
    发明申请
    PROCESS FOR PRODUCING SUBSTITUTED METHYLAMINE COMPOUND AND TRIAZINE DERIVATIVE 审中-公开
    生产取代的甲基胺化合物和三氮唑衍生物的方法

    公开(公告)号：US20140323724A1

    公开(公告)日：2014-10-30

    申请号：US14329356

    申请日：2014-07-11

    申请人： Nippon Soda Co., Ltd.

    发明人： Yasushi SHIBATA ,  Tsutomu IMAGAWA

    IPC分类号： C07D213/61 ,  C07D401/14

    CPC分类号： C07D213/61 ,  C07B43/04 ,  C07C209/06 ,  C07C211/03 ,  C07C211/48 ,  C07C211/62 ,  C07D251/04 ,  C07D257/08 ,  C07D277/20 ,  C07D401/06 ,  C07D401/14 ,  C08G73/0627 ,  C08G73/0644

    摘要： The present invention provides a process that enables a substituted methylamine compound which is useful as an intermediate for the production of agricultural chemicals and medicines, to be produced easily, with good yield, and at low cost, and also provides a production intermediate thereof. The process comprises a step of reacting a hexamethylenetetraammonium salt compound represented by a formula (I) with a base to obtain an N-methylidene-substituted methylamine oligomer represented by a formula (II) or a mixture of two or more of the oligomers, and a step of hydrolyzing the N-methylidene-substituted methylamine oligomer represented by formula (II) or the mixture of two or more of the oligomers in the presence of an acid. (wherein A represents an organic group, R represents a hydrogen atom, or an organic group, L represents a halogen atom and the like, and n represents an integer of 2 to 20)

    摘要翻译： 本发明提供了能够容易地以良好的产率，低成本地制造可用作农药和药品的中间体的取代甲胺化合物的方法，并且还提供其制备中间体。 该方法包括使由式（I）表示的六亚甲基四铵盐化合物与碱反应以获得由式（II）表示的N-亚甲基取代的甲基胺低聚物或两种或更多种低聚物的混合物的步骤，以及 在酸存在下水解由式（II）表示的N-亚甲基取代的甲胺低聚物或两种或更多种低聚物的混合物的步骤。 （其中A表示有机基团，R表示氢原子或有机基团，L表示卤素原子等，n表示2〜20的整数）