Isomerization of β-keto-allenes
    12.
    发明授权
    Isomerization of β-keto-allenes 有权
    异构化和共聚物

    公开(公告)号:US08802898B2

    公开(公告)日:2014-08-12

    申请号:US13642047

    申请日:2011-04-18

    IPC分类号: C07C45/67

    摘要: Isomerization of β-keto-allenes of the general formula I wherein R1 is hydrogen, methyl or ethyl, in particular hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen or methyl, in particular methyl and R4 is an aliphatic hydrocarbon residue containing 1-37 carbon atoms, into corresponding α,γ-dienones of formula II by treatment with a basic ion exchange resin.

    摘要翻译: 其中R 1是氢,甲基或乙基,特别是氢或甲基的通式I的双 - 二烯的异构化; R2是氢或甲基; R3是氢或甲基,特别是甲基,R4是含有1-37个碳原子的脂族烃残基,通过碱性离子交换树脂的处理转化为相应的式II的α,γ-二烯酮。

    Process for the preparation of pyrimidine derivatives
    14.
    发明授权
    Process for the preparation of pyrimidine derivatives 有权
    制备嘧啶衍生物的方法

    公开(公告)号:US08461168B2

    公开(公告)日:2013-06-11

    申请号:US13263142

    申请日:2010-04-08

    IPC分类号: A01N43/54 A61K31/505

    摘要: A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula (I) wherein R is CONH2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H2N CH═C(R)CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula (I) is transferred into an acid addition salt, and the transformation of a compound of formula (II) wherein R is CONH2 into a compound of formula (II) wherein R is CN by treatment with POCI3.

    摘要翻译: 制备其中R为CONH 2或CN的式(I)的5-取代的4-取代的4-氨基-2-甲基嘧啶及其酸加成盐的方法,其特征在于式H 2 N CH = C(R) CN(II)与乙酰亚胺酸甲酯或其酸加成盐反应,如果需要,将式(I)化合物转移到酸加成盐中,并将式(II)化合物转化为其中 R是CONH 2化合物,其中R是通过用POCl 3处理的CN的式(II)化合物。

    PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES
    15.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIMIDINE DERIVATIVES 有权
    制备吡嗪衍生物的方法

    公开(公告)号:US20120095230A1

    公开(公告)日:2012-04-19

    申请号:US13263142

    申请日:2010-04-08

    IPC分类号: C07D239/42 C07C253/20

    摘要: A process for the preparation of 5-substituted 4-amino-2-methylpyrimidines of the formula (I) wherein R is CONH2 or CN, and of acid addition salts thereof, characterized in that a compound of formula H2N CH═C(R) CN (II) is reacted with acetimidic acid methyl ester or an acid addition salt thereof and that, if desired, a compound of formula (I) is transferred into an acid addition salt, and the transformation of a compound of formula (II) wherein R is CONH2 into a compound of formula (II) wherein R is CN by treatment with POCI3.

    摘要翻译: 制备其中R为CONH 2或CN的式(I)的5-取代的4-取代的4-氨基-2-甲基嘧啶及其酸加成盐的方法,其特征在于式H2NCH = CN(II)与乙酰亚胺酸甲酯或其酸加成盐反应,如果需要,将式(I)化合物转移到酸加成盐中,并将式(II)化合物转化为其中 R是CONH 2化合物,其中R是通过用POCl 3处理的CN的式(II)化合物。

    ISOMERIZATION OF BETA-KETO-ALLENES
    18.
    发明申请
    ISOMERIZATION OF BETA-KETO-ALLENES 有权
    BETA-KETO-ALLENES的异构体

    公开(公告)号:US20130197272A1

    公开(公告)日:2013-08-01

    申请号:US13642047

    申请日:2011-04-18

    IPC分类号: C07C45/67

    摘要: Isomerization of β-keto-allenes of the general formula I wherein R1 is hydrogen, methyl or ethyl, in particular hydrogen or methyl; R2 is hydrogen or methyl; R3 is hydrogen or methyl, in particular methyl and R4 is an aliphatic hydrocarbon residue containing 1-37 carbon atoms, into corresponding α,γ-dienones of formula II by treatment with a basic ion exchange resin.

    摘要翻译: 其中R 1是氢,甲基或乙基,特别是氢或甲基的通式I的β-酮 - 双烯异构化; R2是氢或甲基; R3是氢或甲基,特别是甲基,R4是含有1-37个碳原子的脂族烃残基,通过用碱性离子交换树脂处理,转化为相应的式II的α,γ-二烯酮。

    Manufacture of vitamin B6
    19.
    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

    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。

    Manufacture of vitamin b6
    20.
    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

    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< 6>具有良好的效用。