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    Manufacture of vitamin b6
    1.
    发明申请
    Manufacture of vitamin b6 有权
    维生素B6的制造

    公开(公告)号：US20070072254A1

    公开(公告)日：2007-03-29

    申请号：US10579836

    申请日：2004-11-09

    申请人： Jocelyn Fischesser ,  Helmut Fritsch ,  Andrew Gum ,  Reinhard Karge ,  Ralf Keuper

    发明人： Jocelyn Fischesser ,  Helmut Fritsch ,  Andrew Gum ,  Reinhard Karge ,  Ralf Keuper

    IPC分类号： C12Q1/34

    CPC分类号： C07D491/04 ,  Y02P20/582

    摘要： A process for manufacturing a 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 9-acyloxy-1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin (I) and optionally for manufacturing pyridoxine involves performing an addition reaction between a 4-methyl-5-alkoxy-oxazole (II) and a 2-unsubstituted, 2-monosubstituted or 2,2-disubstituted 4,7-dihydro-(1,3)-dioxepin (III) in the substantial absence of a solvent and a catalyst to give a product mixture consisting essentially of the appropriate Diels-Alder adduct (IV) in a major proportion and the appropriate 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin 9-ol (V) in a minor proportion, removal of a substantial proportion of the unreacted oxazole and dioxapin starting materials from the product mixture by distillation under reduced pressure, addition of a substantially anhydrous organic acid to said product mixture and rearrangement of the Diels-Alder adduct IV to further V in the presence of said substantially anhydrous organic acid with removal of the generated alkanol by distillation under reduced pressure, and acylation of the resultingly enriched quantity of V with an added carboxylic acid anhydride to produce the desired I, and optionally converting this so-manufactured acylation product I to pyridoxine by acid hydrolysis for achieving deprotection and deacylatiom. Pyridoxine is a well known form of vitamin B6 with well established utility.

    摘要翻译： 制备3-未取代的3-单取代的或3,3-二取代的9-酰氧基-1,5-二氢-8-甲基吡啶并[3,4-e] [1,3]二氧杂环庚烯（I）的方法， 制备吡哆醛涉及在4-甲基-5-烷氧基 - 恶唑（II）和2-未取代的2-单取代或2,2-二取代的4,7-二氢 - （1,3）二氧杂环己烷 III）在基本上不存在溶剂和催化剂的情况下得到主要比例的基本上由适当的狄尔斯 - 阿尔德加合物（IV）组成的产物混合物和合适的3-未取代的3-单取代的或3,3-二取代的1 ，5-二氢-8-甲基吡啶并[3,4-e] [1,3]二氧杂环庚烷-9-醇（V），从产物混合物中除去大部分未反应的恶唑和二氧杂环己烯起始原料， 在减压下蒸馏，向所述产物混合物中加入基本上无水的有机酸，并将狄尔斯 - 阿尔德加合物IV重新排列成进一步的V 通过在减压下蒸馏除去生成的链烷醇，并用加入的羧酸酐酰化所得的富含量的V以产生所需的I，并且任选地将这样制得的酰化产物I 通过酸水解获得吡哆醛，以实现去保护和脱酰基。 吡哆素是一种众所周知的维生素B 6＆lt; 6＆gt;具有良好的效用。

    Manufacture of vitamin B6
    2.
    发明授权
    Manufacture of vitamin B6 有权
    维生素B6的制造

    公开(公告)号：US07495101B2

    公开(公告)日：2009-02-24

    申请号：US10579836

    申请日：2004-11-09

    申请人： Jocelyn Fischesser ,  Helmut Fritsch ,  Andrew George Gum ,  Reinhard Karge ,  Ralf Keuper

    发明人： Jocelyn Fischesser ,  Helmut Fritsch ,  Andrew George Gum ,  Reinhard Karge ,  Ralf Keuper

    IPC分类号： C07D471/02 ,  C07D491/02 ,  C07D498/02

    CPC分类号： C07D491/04 ,  Y02P20/582

    摘要： A process for manufacturing a 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 9-acyloxy-1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin (I) and optionally for manufacturing pyridoxine involves performing an addition reaction between a 4-methyl-5-alkoxy-oxazole (II) and a 2-unsubstituted, 2-monosubstituted or 2,2-disubstituted 4,7-dihydro-(1,3)-dioxepin (III) in the substantial absence of a solvent and a catalyst to give a product mixture consisting essentially of the appropriate Diels-Alder adduct (IV) in a major proportion and the appropriate 3-unsubstituted, 3-monosubstituted or 3,3-disubstituted 1,5-dihydro-8-methylpyrido[3,4-e] [1,3]dioxepin 9-ol (V) in a minor proportion, removal of a substantial proportion of the unreacted oxazole and dioxapin starting materials from the product mixture by distillation under reduced pressure, addition of a substantially anhydrous organic acid to said product mixture and rearrangement of the Diels-Alder adduct IV to further V in the presence of said substantially anhydrous organic acid with removal of the generated alkanol by distillation under reduced pressure, and acylation of the resultingly enriched quantity of V with an added carboxylic acid anhydride to produce the desired I, and optionally converting this so-manufactured acylation product I to pyridoxine by acid hydrolysis for achieving deprotection and deacylatiom. Pyridoxine is a well known form of vitamin B6 with well established utility.

    摘要翻译： 制备3-未取代的3-单取代的或3,3-二取代的9-酰氧基-1,5-二氢-8-甲基吡啶并[3,4-e] [1,3]二氧杂环庚烯（I）的方法， 制备吡哆醛涉及在4-甲基-5-烷氧基 - 恶唑（II）和2-未取代的2-单取代或2,2-二取代的4,7-二氢 - （1,3）二氧杂环己烷 III）在基本上不存在溶剂和催化剂的情况下得到主要比例的基本上由适当的狄尔斯 - 阿尔德加合物（IV）组成的产物混合物和合适的3-未取代的3-单取代的或3,3-二取代的1 ，5-二氢-8-甲基吡啶并[3,4-e] [1,3]二氧杂环庚烷-9-醇（V），从产物混合物中除去大部分未反应的恶唑和二氧杂环己烯起始原料， 在减压下蒸馏，向所述产物混合物中加入基本上无水的有机酸，并将狄尔斯 - 阿尔德加合物IV重新排列成进一步的V 通过在减压下蒸馏除去生成的链烷醇，并用加入的羧酸酐酰化所得的富含量的V以产生所需的I，并且任选地将这样制得的酰化产物I 通过酸水解获得吡哆醛，以实现去保护和脱酰基。 吡哆素是众所周知的维生素B6形式，具有很好的实用性。

    SYNTHESIS OF 4-AMINO-PYRIMIDINES SCAFFOLDS
    9.
    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。