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公开(公告)号：US20060094886A1
公开(公告)日：2006-05-04
申请号：US10535604
申请日：2003-09-29
申请人： Werner Bonrath , Claus Dittel , Thomas Netscher , Thomas Pabst , Rudolf Schmid
发明人： Werner Bonrath , Claus Dittel , Thomas Netscher , Thomas Pabst , Rudolf Schmid
IPC分类号： C07D311/04 , C07C67/02
CPC分类号： C07D311/72 , C07C67/293 , C07C69/017 , C07C69/16
摘要： A process for the manufacture of 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate, and optionally therefrom tocopheryl acetate, comprises either C-alkylating 2,3,6-trimethylhydroquinone-1-acetate with isophytol or phytol in the presence of a sulphur(VI) containing catalyst of the formula R1SO2OH, wherein R1 signifies hydroxy, halogen, lower alkyl, halogenated lower alkyl or aryl, in an aprotic organic solvent, or O-alkylating 2,3,6-trimethylhydroquinone-1-acetate with a phytyl halide in a polar aprotic organic solvent in the presence of a base, and subjecting the so-obtained 4-O-phytyl-2,3,6-trimethylhydroquinone-1-acetate to a rearrangement reaction, and in each case optionally submitting the so-obtained 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate to a ring closure reaction to produce tocopheryl acetate. The invention also includes the novel compound 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate and certain stereoisomers thereof, and also the further novel compound 4-hydroxy-2,3,6-trimethyl-5-[3-(4,8,12-trimethyltridecyl)-but-3enyl]phenyl acetate which itself is one of several isomers of 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate formed by isomerization under the influence of heating, e.g. during its distillation as part of the isolation and purification procedure following its manufacture as indicated above. (All-rac)-α-tocopherol, which may be derived from its acetate, is known to be the most active industrially important member of the vitamin E group.
摘要翻译： 制备3-植酰基-2,5,6-三甲基氢醌-1-乙酸酯和任选地由其生产生物聚乙酸乙酯的方法包括将2,3,6-三甲基氢醌-1-乙酸酯与间苯二酚或植醇的C-烷基化 含有式R 1 SO 2 OH的含硫（VI）催化剂的存在，其中R 1表示羟基，卤素，低级烷基， 卤代低级烷基或芳基，在非质子有机溶剂中，或在极性非质子有机溶剂中，在碱的存在下，用苄基卤与烷基卤反应，并将如此得到的 4-O-植酰基-2,3,6-三甲基氢醌-1-乙酸酯进行重排反应，并且在每种情况下任选地将如此获得的3-植酰基-2,5,6-三甲基氢醌-1-乙酸酯加入到环中 封闭反应生成醋酸生育酚。 本发明还包括新型化合物3-植酰基-2,5,6-三甲基氢醌-1-乙酸酯及其某些立体异构体，以及另外的新化合物4-羟基-2,3,6-三甲基-5- [3- （4,8,12-三甲基十三烷基） - 丁烯基]苯基乙酸酯，其本身是在加热的影响下通过异构化形成的3-植酰基-2,5,6-三甲基氢醌-1-乙酸酯的几种异构体之一，例如 在其蒸馏期间作为如上所述的其制造之后的分离和纯化方法的一部分。 （全 - 外消旋）-α-生育酚可以衍生自其乙酸酯已知是维生素E组中最活跃的工业上重要的成员。
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32.发明申请Process for the manufacture of chroman derivatives, especially alpha-tocopherol and alkanoates thereof 审中-公开苯并二氢吡喃衍生物，特别是α-生育酚及其链烷酸酯的制备方法公开(公告)号：US20050277777A1
公开(公告)日：2005-12-15
申请号：US11005113
申请日：2004-12-06
IPC分类号： C07D311/00 , C07D311/72 , C07D311/74
CPC分类号： C07D311/72
摘要： The present invention relates to novel processes for the manufacture of chroman derivatives such as α-tocopherol (TCP) and alkanoates thereof, especially α-tocopheryl acetate (TCPA), whereby at least one step of the processes is carried out in the presence of a Lewis acid or a mixture of a Lewis acid with a Bronsted acid as the catalyst under pressure, preferably at an absolute pressure of at least 1.1 bar. As starting materials for the manufacture of TCP and its alkanoates either a mixture of 2,3,5-trimethylhydroquinone (TMHQ) or 2,3,6-trimethylhydroquinone-1-alkanoate (TMHQA) and a compound selected from the group consisting of phytol (pH), isophytol (IP) and (iso)phytol derivatives or 2-phytyl-3,5,6-trimethyl-hydroquinone (PTMHQ)/3-phytyl-2,5,6-trimethylhydroquinone-1-alkanoate (PTMHQA) and/or an isomer thereof are used. Suitable Lewis acids are indium(III) salts and scandium(III) salts. Suitable acid mixtures are iron/iron(II) chloride/hydrogen chloride and zinc(II) chloride/hydrogen chloride.
摘要翻译： 本发明涉及制造色氨酸衍生物如α-生育酚（TCP）及其链烷酸酯，特别是α-生育酚乙酸酯（TCPA）的新方法，其中至少一个步骤的方法是在 路易斯酸或路易斯酸与布朗斯台德酸的混合物作为催化剂，优选在至少1.1巴的绝对压力下进行。 作为制备TCP及其链烷酸酯的起始原料是2,3,5-三甲基氢醌（TMHQ）或2,3,6-三甲基氢醌-1-链烷酸酯（TMHQA）的混合物和选自植醇 （pH），异植醇（IP）和（异）植醇衍生物或2-植酰基-3,5,6-三甲基 - 氢醌（PTMHQ）/ 3-植酰基-2,5,6-三甲基氢醌-1-链烷酸酯（PTMHQA） 和/或其异构体。 合适的路易斯酸是铟（III）盐和钪（III）盐。 合适的酸混合物是氯化铁/氯化铁（II）/氯化氢和氯化锌（II）/氯化氢。
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公开(公告)号：US06700002B2
公开(公告)日：2004-03-02
申请号：US10053297
申请日：2002-01-17
IPC分类号： C07D31108
CPC分类号： C07D311/72
摘要： A process for the manufacture of (all-rac)-&agr;-tocopherol by the catalyzed reaction of trimethylhydroquinone with isophytol or phytol is characterized by carrying out the reaction in the presence of hydrogen tris(oxalato)phosphate, or an adduct thereof with a solvent, as the catalyst in an organic solvent. The product of the process is the most active and industrially most important member of the vitamin E group.
摘要翻译： 通过三甲基氢醌与异植醇或植醇的催化反应制备（全脱色）-α-生育酚的方法的特征在于在三（草酸）磷酸氢盐或其与溶剂的加合物存在下进行反应 作为有机溶剂中的催化剂。 该过程的产物是维生素E组中最活跃和最具工业最重要的成员。
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34.发明授权Process of separating chiral isomers of chroman compounds and their derivatives and precursors 有权分离色满化合物及其衍生物和前体的手性异构体的方法公开(公告)号：US08987480B2
公开(公告)日：2015-03-24
申请号：US14116880
申请日：2012-05-08
IPC分类号： C07D311/76 , C07D311/04 , C07B55/00 , C07B57/00 , C07D311/22 , C07D311/72
CPC分类号： C07D311/04 , C07B55/00 , C07B57/00 , C07D311/22 , C07D311/72
摘要： The present invention relates to a process of separating chiral isomers of chroman compounds, particularly tocopherols and tocotrienols as well as the esters and intermediates thereof. It has been found that this process allows a separation of the desired isomer with a higher yield and enables the use of the non-desired isomers in a very efficient way. Said process is particularly useful when implemented in an industrial process. Furthermore, it has been found that this process allows using isomer mixtures as they result from traditional industrial synthesis.
摘要翻译： 本发明涉及分离苯并二氢吡喃化合物，特别是生育酚和生育三烯酚的手性异构体及其酯和中间体的方法。 已经发现，该方法允许以更高的产率分离所需的异构体，并且能够以非常有效的方式使用非期望的异构体。 当在工业过程中实施时，所述方法特别有用。 此外，已经发现，该方法允许使用由传统工业合成得到的异构体混合物。
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公开(公告)号：US5892058A
公开(公告)日：1999-04-06
申请号：US848041
申请日：1997-04-28
IPC分类号： B01J21/02 , C07B61/00 , C07D311/72 , C07D311/04
CPC分类号： C07D311/72 , Y02P20/582
摘要： A method of producing .alpha.-tocopherol from non-.alpha.-tocopherols is disclosed. In the disclosed method, non-.alpha.-tocopherols are hydroxymethylated and reduced to .alpha.-tocopherol in a single step by reacting formaldehyde or a formaldehyde-producing compound with the non-.alpha.-tocopherol under catalytic reducing conditions in a reaction mixture containing the non-.alpha.-tocopherol, formaldehyde or formaldehyde-producing compound and boric acid or a boric acid-producing compound dispersed in a solvent of an azeotropic mixture of trimethyl borate and methanol and a non-polar organic solvent.
摘要翻译： 公开了一种从非α-生育酚生产α-生育酚的方法。 在所公开的方法中，非α-生育酚被羟甲基化并在一个步骤中通过使甲醛或产生甲醛的化合物与非α-生育酚在催化还原条件下在含有非α-生育酚的反应混合物中反应而被还原成α-生育酚， α-生育酚，甲醛或生产甲醛的化合物和分散在硼酸三甲酯和甲醇和非极性有机溶剂的共沸混合物的溶剂中的硼酸或硼酸生成化合物。
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36.发明申请PROCESS OF SEPARATING CHIRAL ISOMERS OF CHROMAN COMPOUNDS AND THEIR DERIVATIVES AND PRECURSORS 有权分离化合物及其衍生物和前体的化学物质的分离方法公开(公告)号：US20140155636A1
公开(公告)日：2014-06-05
申请号：US14116880
申请日：2012-05-08
IPC分类号： C07D311/04
CPC分类号： C07D311/04 , C07B55/00 , C07B57/00 , C07D311/22 , C07D311/72
摘要： The present invention relates to a process of separating chiral isomers of chroman compounds, particularly tocopherols and tocotrienols as well as the esters and intermediates thereof. It has been found that this process allows a separation of the desired isomer with a higher yield and enables the use of the non-desired isomers in a very efficient way. Said process is particularly useful when implemented in an industrial process. Furthermore, it has been found that this process allows using isomer mixtures as they result from traditional industrial synthesis.
摘要翻译： 本发明涉及分离苯并二氢吡喃化合物，特别是生育酚和生育三烯酚的手性异构体及其酯和中间体的方法。 已经发现，该方法允许以更高的产率分离所需的异构体，并且能够以非常有效的方式使用非期望的异构体。 当在工业过程中实施时，所述方法特别有用。 此外，已经发现，该方法允许使用由传统工业合成得到的异构体混合物。
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公开(公告)号：US20080194417A1
公开(公告)日：2008-08-14
申请号：US11885665
申请日：2006-02-28
IPC分类号： C40B30/04
CPC分类号： C12Q1/6876 , C12Q2600/136 , C12Q2600/158
摘要： Biologically active compounds (e.g. from the groups of pharmaceutical drugs, cofactors, hormones, vitamins or phytochemicals) often consist of two or more stereoisomers (enantiomers or diastereoisomers) which may differ in their pharmacodynamic/kinetic, toxicological and biological properties. These differences are so far difficult to detect. A well known example for a biologically active compound and its counterpart is vitamin E which is predominantly administered as two different ‘forms’, one derived from natural sources (mainly soybeans), and one from production by chemical total-synthesis. While vitamin E from natural sources occurs as a single stereoisomer (RRR-α-tocopherol), so-called synthetic vitamin E (all-rac-α-tocopherol) is an equimolar mixture of eight stereoisomers. The present invention is directed to a method for calculating the biological activity of a biologically active compound (e.g. RRR-α-tocopherol) and a counterpart thereof (e.g. all-rac-α-tocopherol), comprising the steps of: culturing a plurality of cells in a culture medium and treating the cells with different concentrations of either said compound or said counterpart thereof; or treating a plurality of animals or plants with different concentrations of either said compound or said counterpart; preparing samples from the treated cells or animals or plants containing a pool of target nucleic acids comprising RNA transcripts; detecting the expression of genes in said cells by measuring the amount of transcripts of said genes to obtain a target expression pattern by hybridizing said pool of target nucleic acids to an array of nucleic acid probes immobilized on a surface, wherein said array comprising at least 10 different nucleic acids, some of which comprise control probes, and wherein each different nucleic acid is localized in a known location of said surface; quantifying the hybridization of said nucleic acids to said array by comparing binding of matched and control probes; calculating the biological activity of the compound and its counterpart therefrom.
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