Process for producing vitamin A ester
    1.
    发明授权
    Process for producing vitamin A ester 有权
    生产维生素A酯的方法

    公开(公告)号:US06727381B2

    公开(公告)日:2004-04-27

    申请号:US10039056

    申请日:2002-01-03

    IPC分类号: C07C6702

    摘要: The invention relates to a process for producing all trans-vitamin A ester (I). According to the present invention, vitamin A ester (I) can simply be synthesized in good yields and high purity by the reaction of phosphonate compound (IV) with aldehyde (II) in an organic solvent in the presence of a base.

    摘要翻译: 本发明涉及一种生产全部维生素A酯(I)的方法。 根据本发明,通过膦酸酯化合物(IV)与醛(II)在有机溶剂中在碱的存在下的反应,可以简单地以高产率和高纯度合成维生素A酯(I)。

    Method of preparing 2,6,10-Trimethyl-1,1-dialkoxy-3,5,9-undecatriene used as an intermediate of lycopene
    2.
    发明授权
    Method of preparing 2,6,10-Trimethyl-1,1-dialkoxy-3,5,9-undecatriene used as an intermediate of lycopene 有权
    制备用作番茄红素中间体的2,6,10-三甲基-1,1-二烷氧基-3,5,9-十一碳三烯的方法

    公开(公告)号:US09051254B2

    公开(公告)日:2015-06-09

    申请号:US13493971

    申请日:2012-06-11

    IPC分类号: C07C41/01 C07C41/48

    CPC分类号: C07C41/48 C07C43/303

    摘要: The present invention describes a novel synthetic method for preparing the key intermediate 2,6,10-trimethyl-1,1-dialkoxy-3,5,9-undecatriene of lycopene. An existing synthetic method have some disadvantages that it is very difficult to gain the raw material dialkyl 4-methyl-5,5-diakoxy-1-pentene-1-phosphonate (10) because no effective synthetic method can be adopted, and furthermore the obtained target compound is composed of several cis/trans isomers. This invention relates to a process comprising a condensation step wherein a starting C10-phosphonate is changed to its carbanion completely at a temperature of −40˜30 under an atmosphere of a non-reactive gas in an organic solvent catalyzed by base, and then C4-dialkyl is added to undergo Wittig-Horner condensation. This invention affords all trans C14-acetal and this method is characterized with the advantages of simple procedure, easy access to raw material and low cost, which makes it has the value of industrial application.

    摘要翻译: 本发明描述了一种制备番茄红素关键中间体2,6,10-三甲基-1,1-二烷氧基-3,5,9-十一碳三烯的新型合成方法。 现有的合成方法有一些缺点,因为没有有效的合成方法,难以获得原料的4-甲基-5,5-二烷氧基-1-戊烯-1-膦酸二烷基酯(10),此外, 得到的目标化合物由几种顺式/反式异构体组成。 本发明涉及一种包括缩合步骤的方法,其中起始C10-膦酸酯在-40〜30℃的温度下在非反应性气体的气氛中在由碱催化的有机溶剂中完全变成其碳负离子,然后将C4 加入二烷基以进行Wittig-Horner冷凝。 本发明提供全反式C14-缩醛,该方法的特点是操作简单,易于获得原料,成本低廉,具有工业应用价值。

    Lycopene Intermediate 1, 3, 6, 10-Tetra-Double Bond Pentadec-Carbon Phosphonate as well as Preparation Method and Use Thereof
    3.
    发明申请
    Lycopene Intermediate 1, 3, 6, 10-Tetra-Double Bond Pentadec-Carbon Phosphonate as well as Preparation Method and Use Thereof 有权
    番茄红素中间体1,3,6,10-四 - 双键十五碳膦酸酯及其制备方法和用途

    公开(公告)号:US20120330048A1

    公开(公告)日:2012-12-27

    申请号:US13583635

    申请日:2011-03-09

    IPC分类号: C07F9/40

    CPC分类号: C07F9/4015

    摘要: The invention relates to a novel important lycopene intermediate 3,7, 11-trimethyl-1,3,6,10-tetraene-dodecyl diethyl phosphonate. A current lycopene intermediate 2,4,6,10-tetra-double bond pentadec-carbon phosphonate is difficult to synthesize. The invention provides a novel intermediate, which has the following synthesis steps of: preparing 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde from pseudoionone; preparing 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde from the 2,6,10-trimethyl-3, 5,9-undecane triene-1-aldehyde; and subjecting the 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde and tetraethyl methylenediphosphonate to condensation reaction to obtain target product. The invention can generate novel intermediate from raw material pseudoionone only by four reactions, thus the reactions are easy to control and great industrial value are achieved.

    摘要翻译: 本发明涉及一种新型重要的番茄红素中间体3,7,11-三甲基-1,3,6,10-四烯十二烷基二乙基膦酸酯。 目前的番茄红素中间体2,4,6,10-四 - 双十五碳酸膦难以合成。 本发明提供了一种新的中间体,其具有以下合成步骤:由假雄酮制备2,6,10-三甲基-3,5,9-十一烷三烯-1-醛; 由2,6,10-三甲基-3,9,9-十一烷三烯-1-醛制备2,6,10-三甲基-2,5,9-十一烷三烯-1-醛; 并使2,6,10-三甲基-2,5,9-十一烷三烯-1-醛和四亚乙基二膦酸四乙酯进行缩合反应,得到目标产物。 本发明只能通过四个反应从原料假雄酮生成新的中间体,因此反应易于控制,实现了巨大的工业价值。

    Lycopene intermediate 1, 3, 6, 10-tetra-double bond pentadec-carbon phosphonate as well as preparation method and use thereof
    4.
    发明授权
    Lycopene intermediate 1, 3, 6, 10-tetra-double bond pentadec-carbon phosphonate as well as preparation method and use thereof 有权
    番茄红素中间体1,3,6,10-四 - 双十五碳酸膦酸酯及其制备方法和用途

    公开(公告)号:US08765988B2

    公开(公告)日:2014-07-01

    申请号:US13583635

    申请日:2011-03-09

    IPC分类号: C07F9/40

    CPC分类号: C07F9/4015

    摘要: The invention relates to a novel important lycopene intermediate 3,7,11-trimethyl-1,3,6,10-tetraene-dodecyl diethyl phosphonate. A current lycopene intermediate 2,4,6,10-tetra-double bond pentadec-carbon phosphonate is difficult to synthesize. The invention provides a novel intermediate, which has the following synthesis steps of: preparing 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde from pseudoionone; preparing 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde from the 2,6,10-trimethyl-3,5,9-undecane triene-1-aldehyde; and subjecting the 2,6,10-trimethyl-2,5,9-undecane triene-1-aldehyde and tetraethyl methylenediphosphonate to condensation reaction to obtain target product. The invention can generate novel intermediate from raw material pseudoionone only by four reactions, thus the reactions are easy to control and great industrial value are achieved.

    摘要翻译: 本发明涉及新型重要的番茄红素中间体3,7,11-三甲基-1,3,6,10-四烯十二烷基二乙基膦酸酯。 目前的番茄红素中间体2,4,6,10-四 - 双十五碳酸膦难以合成。 本发明提供了一种新的中间体,其具有以下合成步骤:由假雄酮制备2,6,10-三甲基-3,5,9-十一烷三烯-1-醛; 由2,6,10-三甲基-3,5,9-十一烷三烯-1-醛制备2,6,10-三甲基-2,5,9-十一烷三烯-1-醛; 并使2,6,10-三甲基-2,5,9-十一烷三烯-1-醛和四亚乙基二膦酸四乙酯进行缩合反应,得到目标产物。 本发明只能通过四个反应从原料假雄酮生成新的中间体,因此反应易于控制,实现了巨大的工业价值。

    LINEZOLID INTERMEDIATE AND METHOD FOR SYNTHESIZING LINEZOLID
    8.
    发明申请
    LINEZOLID INTERMEDIATE AND METHOD FOR SYNTHESIZING LINEZOLID 有权
    LINEZOLID中间体和用于合成LINEZOLID的方法

    公开(公告)号:US20140024827A1

    公开(公告)日:2014-01-23

    申请号:US14008124

    申请日:2012-04-12

    摘要: Provided are a linezolid intermediate and the preparation method thereof and a method for synthesizing linezolid. The structure of the intermediate is shown as formula F2, wherein the compound is prepared by a condensation reaction of (S)—N—(3-chloro-2-hydroxy-1-propyl) acetamide and the compound shown in formula F4. In the preparation methods of the compound shown in formula F2 and linezolid, the reaction system is mild, side reactions are few and the product yield is high.

    摘要翻译: 提供了一种利奈唑胺中间体及其制备方法和合成利奈唑胺的方法。 中间体的结构如式F2所示,其中化合物通过(S)-N-(3-氯-2-羟基-1-丙基)乙酰胺与式F4所示的化合物的缩合反应制备。 在式F2和利奈唑胺的化合物的制备方法中,反应体系温和,副反应少,产物收率高。

    Method of Preparing 2,6,10-Trimethyl-1,1-Dialkoxy-3,5,9-Undecatriene Used as an Intermediate of Lycopene
    9.
    发明申请
    Method of Preparing 2,6,10-Trimethyl-1,1-Dialkoxy-3,5,9-Undecatriene Used as an Intermediate of Lycopene 有权
    制备用作番茄红素中间体的2,6,10-三甲基-1,1-二烷氧基-3,5,9-十一碳三烯的方法

    公开(公告)号:US20120316366A1

    公开(公告)日:2012-12-13

    申请号:US13493971

    申请日:2012-06-11

    IPC分类号: C07C41/01

    CPC分类号: C07C41/48 C07C43/303

    摘要: The present invention describes a novel synthetic method for preparing the key intermediate 2,6,10-trimethyl-1,1-dialkoxy-3,5,9-undecatriene of lycopene. An existing synthetic method have some disadvantages that it is very difficult to gain the raw material dialkyl 4-methyl-5,5-diakoxy-1-pentene-1-phosphonate (10) because no effective synthetic method can be adopted, and furthermore the obtained target compound is composed of several cis/trans isomers. This invention relates to a process comprising a condensation step wherein a starting C10-phosphonate is changed to its carbanion completely at a temperature of −40˜30 under an atmosphere of a non-reactive gas in an organic solvent catalyzed by base, and then C4-dialkyl is added to undergo Wittig-Horner condensation. This invention affords all trans C14-acetal and this method is characterized with the advantages of simple procedure, easy access to raw material and low cost, which makes it has the value of industrial application.

    摘要翻译: 本发明描述了一种制备番茄红素关键中间体2,6,10-三甲基-1,1-二烷氧基-3,5,9-十一碳三烯的新型合成方法。 现有的合成方法有一些缺点,因为没有有效的合成方法,难以获得原料的4-甲基-5,5-二烷氧基-1-戊烯-1-膦酸二烷基酯(10),此外, 得到的目标化合物由几种顺式/反式异构体组成。 本发明涉及一种包括缩合步骤的方法,其中起始C10-膦酸酯在-40〜30℃的温度下在非反应性气体的气氛中在由碱催化的有机溶剂中完全变成其碳负离子,然后将C4 加入二烷基以进行Wittig-Horner冷凝。 本发明提供全反式C14-缩醛,该方法的特点是操作简单,易于获得原料,成本低廉,具有工业应用价值。

    1-methoxyl-2, 6, 10-trimethyl-1, 3, 5, 9-undec-tetraene, and preparation method and uses thereof
    10.
    发明授权
    1-methoxyl-2, 6, 10-trimethyl-1, 3, 5, 9-undec-tetraene, and preparation method and uses thereof 有权
    1-甲氧基-2,6,10-三甲基-1,3,5,9-十一四烯及其制备方法和用途

    公开(公告)号:US08697919B2

    公开(公告)日:2014-04-15

    申请号:US13639852

    申请日:2011-04-06

    IPC分类号: C07C45/42 C07C41/30 C07C43/15

    摘要: The invention discloses an intermediate 1-methoxyl-2,6,10-trimethyl-1,3,5, 9-undec-tetraene, and a preparation method and uses thereof. In the synthesis method for the current lycopene intermediate 2-pos double bond C-14 aldehyde (2,6,10-trimethyl-2,5,9-undecatriene-1-aldehyde), expensive methyl iodide, polluting dimethyl sulphide and dangerous strong base are needed, so that the method is hardly applied to industrial production. The invention provides a new compound 1-methoxyl-2,6,10-trimethyl-1,3,5,9-undec-tetraene, and pure 2-pos double bond C-14 aldehyde can be prepared by hydrolyzing and refining the compound. The synthetic route is simplified and the great suitability for industrial production is achieved.

    摘要翻译: 本发明公开了中间体1-甲氧基-2,6,10-三甲基-1,3,5,9-十一四烯及其制备方法和用途。 在目前番茄红素中间体2-pos双键C-14醛(2,6,10-三甲基-2,5,9-十一碳三烯-1-醛)的合成方法中,昂贵的甲基碘,污染二甲基硫化物和危险的强 需要这种方法,这种方法几乎不适用于工业生产。 本发明提供了一种新的化合物1-甲氧基-2,6,10-三甲基-1,3,5,9-十一四烯,纯的2-位双键C-14醛可以通过水解和精制化合物 。 合成路线简化,实现了工业生产的良好适应性。