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    NOVEL SYNTHESIS OF SUBSTITUTED 4-AMINO-PYRIMIDINES
    1.
    发明申请
    NOVEL SYNTHESIS OF SUBSTITUTED 4-AMINO-PYRIMIDINES 有权
    取代的4-氨基吡啶的新合成

    公开(公告)号：US20110178300A1

    公开(公告)日：2011-07-21

    申请号：US13055579

    申请日：2009-07-22

    申请人： Reinhard Karge ,  Ulla Letinois ,  Gerhard Shiefer

    发明人： Reinhard Karge ,  Ulla Letinois ,  Gerhard Shiefer

    IPC分类号： C07D239/42 ,  C07C211/22

    CPC分类号： C07C255/30 ,  C07C271/20 ,  Y02P20/55

    摘要： The present invention is directed to a process for the manufacture of compounds of formula IV wherein R1 is an amino protecting group, and R2 is hydrogen or C1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M+ is a cation, preferably selected from the group consisting of Li+, Na+, K+, ms, ½ Mg2+ and ½ Zn2+, (formula 1a) with an ammonium salt NH4X−, wherein X− is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R2—CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B1.

    摘要翻译： 本发明涉及制备式IV化合物的方法，其中R 1是氨基保护基，R 2是氢或C 1-10烷基，其包括a）使式Ia化合物（其中M +是阳离子） 优选选自Li +，Na +，K +，ms，½Mg2 +和½Zn2 +，（式1a）与铵盐NH4X-，其中X是阴离子，优选选自氯化物，溴化物， 硫酸盐和乙酸盐，在溶剂中与式Ⅱ化合物反应b）使式Ⅱ化合物与腈R2-CN在碱的存在下反应于式Ⅳ化合物。 本发明还涉及式II化合物及其制备维生素B1的用途。

    Synthesis of substituted 4-amino-pyrimidines
    2.
    发明授权
    Synthesis of substituted 4-amino-pyrimidines 有权
    取代的4-氨基 - 嘧啶的合成

    公开(公告)号：US08252927B2

    公开(公告)日：2012-08-28

    申请号：US13055579

    申请日：2009-07-22

    申请人： Reinhard Karge ,  Ulla Letinois ,  Gerhard Shiefer

    发明人： Reinhard Karge ,  Ulla Letinois ,  Gerhard Shiefer

    IPC分类号： C07D239/02

    CPC分类号： C07C255/30 ,  C07C271/20 ,  Y02P20/55

    摘要： The present invention is directed to a process for the manufacture of compounds of formula IV wherein R1 is an amino protecting group, and R2 is hydrogen or C1-10 alkyl, comprising a) reacting a compound of formula Ia, wherein M+ is a cation, preferably selected from the group consisting of Li+, Na+, K+, ½ Mg2+ and ½ Zn2+, (formula 1a) with an ammonium salt NH4+X−, wherein X− is an anion, preferably selected from the group consisting of chloride, bromide, sulfate and acetate, in a solvent to a compound of formula II b) reacting a compound of formula II with a nitrile R2—CN in the presence of a base to a compound of formula IV. The present invention is further directed to compounds of formula II and their use for the manufacture of vitamin B1.

    摘要翻译： 本发明涉及制备式IV化合物的方法，其中R 1是氨基保护基，R 2是氢或C 1-10烷基，其包括a）使式Ia化合物（其中M +是阳离子） 优选选自Li +，Na +，K +，1 / Mg 2 +和1/2 Zn 2+，（式1a）与铵盐NH 4 + X-，其中X是阴离子，优选选自氯化物，溴化物， 硫酸盐和乙酸盐，在溶剂中与式Ⅱ化合物反应b）使式Ⅱ化合物与腈R2-CN在碱的存在下反应于式Ⅳ化合物。 本发明还涉及式II化合物及其制备维生素B1的用途。

    SYNTHESIS OF 4-AMINO-PYRIMIDINES SCAFFOLDS
    3.
    发明申请
    SYNTHESIS OF 4-AMINO-PYRIMIDINES SCAFFOLDS 有权
    合成4-氨基吡啶类化合物

    公开(公告)号：US20100016591A1

    公开(公告)日：2010-01-21

    申请号：US12522929

    申请日：2008-01-17

    申请人： Werner Bonrath ,  Ralph Haerter ,  Reinhard Karge ,  Ulla Letinois

    发明人： Werner Bonrath ,  Ralph Haerter ,  Reinhard Karge ,  Ulla Letinois

    IPC分类号： C07D239/42

    CPC分类号： C07D239/42

    摘要： Process for the manufacture of a compound of the structure (I) with R1=hydrogen, alkyl (C1-C10, linear, cyclic or branched, aliphatic or aromatic), NR′R″ (wherein R′ and R″ are independently selected from H, alkyl [C1-C10, linear, cyclic or branched, aliphatic or aromatic] and R2=CH2R3 wherein R3 is selected from NHR1′″ (with R′″=C(O)H, C(O)CH3, C(O)alkyl, CH2C6H2(OMe)3 or other saponifiable residues), alkyl (C1-C10, linear, cyclic or branched) aromatic residues, heteroaryl residues, substituted aryl residues, e.g. 3,4,5-trimethoxy-phenyl) wherein 1 equivalent of an α-formyl-propionitrile salt is reacted with 0.75 to 2 equivalents of an acetamidine salt in the presence of a Lewis acid.

    摘要翻译： 制备具有R 1 =氢，（C 1 -C 10，直链，环状或支链，脂族或芳族）烷基的结构（I）的化合物的方法，NR'R“（其中R'和R”独立地 选自H，烷基[C1-C10，直链，支链或支链，脂族或芳族]和R2 = CH2R3，其中R3选自NHR1“（其中R”'= C（O）H，C（O） CH3，C（O）烷基，CH2C6H2（OMe）3或其他可皂化残基），烷基（C1-C10，直链，环状或支链）芳族残基，杂芳基残基，取代的芳基，例如3,4,5-三甲氧基 - 苯基），其中1当量的α-甲酰基 - 丙腈盐与路易斯酸存在下的0.75至2当量的乙脒盐反应。

    Synthesis of 4-amino-pyrimidines scaffolds
    4.
    发明授权
    Synthesis of 4-amino-pyrimidines scaffolds 有权
    合成4-氨基 - 嘧啶支架

    公开(公告)号：US08198443B2

    公开(公告)日：2012-06-12

    申请号：US12522929

    申请日：2008-01-07

    申请人： Werner Bonrath ,  Ralph Haerter ,  Reinhard Karge ,  Ulla Letinois

    发明人： Werner Bonrath ,  Ralph Haerter ,  Reinhard Karge ,  Ulla Letinois

    IPC分类号： C07D239/02

    CPC分类号： C07D239/42

    摘要： Process for the manufacture of a compound of the structure (I) with R1=hydrogen, alkyl (C1-C10, linear, cyclic or branched, aliphatic or aromatic), NR′R″ (wherein R′ and R″ are independently selected from H, alkyl [C1-C10, linear, cyclic or branched, aliphatic or aromatic] and R2=CH2R3 wherein R3 is selected from NHR1′″ (with R′″=C(O)H, C(O)CH3, C(O)alkyl, CH2C6H2(OMe)3 or other saponifiable residues), alkyl (C1-C10, linear, cyclic or branched) aromatic residues, heteroaryl residues, substituted aryl residues, e.g. 3,4,5-trimethoxy-phenyl) wherein 1 equivalent of an α-formyl-propionitrile salt is reacted with 0.75 to 2 equivalents of an acetamidine salt in the presence of a Lewis acid.

    摘要翻译： 制备具有R1 =氢，（C1-C10，直链，环状或支链，脂族或芳族）烷基的结构（I）的化合物的方法，NR'R“（其中R'和R”独立地选自 H，烷基[C1-C10，直链，环状或支链的脂族或芳族]和R2 = CH2R3，其中R3选自NHR1“（其中R'”= C（O）H，C（O） O）烷基，CH 2 C 6 H 2（OMe）3或其他可皂化残基），烷基（C 1 -C 10，直链，环状或支链）芳族残基，杂芳基残基，取代的芳基，例如3,4,5-三甲氧基 - 苯基），其中1 在路易斯酸存在下，将相当于α-甲酰基 - 丙腈盐与0.75至2当量的乙脒盐反应。