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1. 发明申请

US20080242863A1 Process For the Manufacture of a Precursor of Vitamin B1 有权
标题翻译：制造维生素B1前体的方法
公开(公告)号：US20080242863A1
公开(公告)日：2008-10-02
申请号：US11795957
申请日：2006-01-24
申请人： Werner Bonrath , Jocelyn Fischesser , Lisa Giraudi , Reinhard Karge
发明人： Werner Bonrath , Jocelyn Fischesser , Lisa Giraudi , Reinhard Karge
IPC分类号： C07D417/06 , C07D239/94
CPC分类号： C07D239/42 , C07D417/06
摘要： The present invention relates to a novel process for the manufacture of Grewe-diamine comprising the following step: hydrolyzing a compound of formula (II), wherein R is hydrogen or straight- or branched chain C1-4 alkyl, with an aqueous alkali or alkaline-earth metal hydroxide solution, characterized in that the hydrolysis is carried out in the presence of an organic solvent.
摘要翻译：本发明涉及一种制备Grewe-二胺的新方法，包括以下步骤：将式（II）化合物（其中R是氢或直链或支链C 1-4烷基）与碱或碱水溶液水解 - 碱金属氢氧化物溶液，其特征在于水解是在有机溶剂的存在下进行的。

2. 发明申请

US20060293529A1 Process for the manufacture of tocyl and tocopheryl acylates 有权
标题翻译：制备辛酰基和生育酚酰化物的方法
公开(公告)号：US20060293529A1
公开(公告)日：2006-12-28
申请号：US10554885
申请日：2004-04-27
申请人： Werner Bonrath , Lisa Giraudi
发明人： Werner Bonrath , Lisa Giraudi
IPC分类号： C07D311/02
CPC分类号： C07D311/72
摘要： A process for the manufacture of a tocyl acylate or a tocopheryl acylate comprises reacting tocol or a tocopherol with an acylating agent in the presence of a solid heterogeneous Brönsted acid catalyst, said catalyst being an inorganic Brönsted acid on a solid carrier material which comprises silicon dioxide, titanium dioxide or both silicon dioxide and titanium dioxide, or being an organofunctional polysilonaxe featuring sulpho groups, the solid heterogeneous Brönsted acid catalyst further featuring a BET surface area from about 10 m2/g to about 800 m2/g and a pore volume from about 0.1 ml/g to about 2.0 ml/g. The main commercial form of vitamin E, being (all-rac)-α-tocopheryl acetate, can be manufactured by acylation of (all-rac)-α-tocopherol according to this process.
摘要翻译：制备酰基酰化物或生育酚酰基化物的方法包括在固体异质布朗斯台德酸催化剂存在下，将酰基转化成醇或生育酚，所述催化剂是固体载体材料上的无机布朗斯台德酸，其包含二氧化硅，二氧化钛或二氧化硅二氧化钛，或者是具有硫酸基的有机官能聚异氰酸酯，该固体异质布朗斯台德酸催化剂还具有约10m 2 / g至约800μm的BET表面积 2 / g，孔体积为约0.1ml / g至约2.0ml / g。维生素E的主要商业形式是（全脱氧）-α-生育酚乙酸酯，可以通过根据该方法酰化（全 - 外消旋）-α-生育酚来制备。

3. 发明授权

US07135580B2 Process for the manufacture of α-tocopheryl acetate 有权
标题翻译：制备α-生育酚乙酸酯的方法
公开(公告)号：US07135580B2
公开(公告)日：2006-11-14
申请号：US10541360
申请日：2003-12-22
申请人： Werner Bonrath , Claus Dittel , Lisa Giraudi , Thomas Netscher , Thomas Pabst
发明人： Werner Bonrath , Claus Dittel , Lisa Giraudi , Thomas Netscher , Thomas Pabst
IPC分类号： C07D311/72
CPC分类号： C07D311/72
摘要： The present invention is concerned with a novel process for the manufacture of α-tocopheryl acetate which comprises reacting 2,3,6-trimethylhydroquinone-1-acetate with a compound selected from the group consisting of phytol (formula IV with R═OH), iso-phytol (formula III with R═OH), and (iso) phytol derivatives represented by the following formulae III and IV with R═C2-to C5-alkonoyloxy, benzoyloxy, mesyloxy, bezenesul-fonyloxy or tosyloxy, (IV) in the presence of a catalyst of the formula Mn+(R1SO3−)n, wherein Mn+ is a silver, copper, gallium, hafnium or rare earth metal cation, n is the valence of the cation Mn+, and R1 is fluorine, C1-8-perfluoroalkyl or perfluoroaryl, and, if required, cyclizing any 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate or a double bond isomer thereof obtained as an intermediate reaction product, to produce α-tocopheryl acetate. In the catalyst Mn+ is preferably Ag+, Cu+, Ga3+, Sc3+, Lu3+, Ho3+, Tm3+, Yb3+ or Hf4+.
摘要翻译：本发明涉及制备乙酸α-生育酚酯的新方法，其包括使2,3,6-三甲基氢醌-1-乙酸酯与选自植醇（式IV与R-OH）的化合物反应，异山嵛醇（具有R-OH的式III）和由下式III和IV表示的（iso）植醇醇衍生物，其具有至少2个至5个C 5 - 烷酰氧基，苯甲酰氧基，甲磺酰氧基，枯烯二烯基氧基或甲苯磺酰氧基，（Ⅳ）在式M n n n a a a>>>>>>>>>>>>>>>>>>>>>>>>>> 其中M + N +是银，铜，镓，铪或稀土金属阳离子，n是阳离子的化合价 M + N +，R 1是氟，C 1-8 - 全氟烷基或全氟芳基，如果需要，可以将任何3-植酰基 - 获得的作为中间体反应产物的2,5,6-三甲基氢醌-1-乙酸酯或其双键异构体，以产生乙酸α-生育酚酯。在催化剂中，N + +优选为Ag +，Cu +，Ga 3+，Sc 3 或+ 3+，3+，3 +，3 +，3 +，3 + Hf 4+。

4. 发明申请

US20060052618A1 Process for the manufacture of alpha-tocopheryl acetate 有权
标题翻译：制备α-生育酚乙酸酯的方法
公开(公告)号：US20060052618A1
公开(公告)日：2006-03-09
申请号：US10541360
申请日：2003-12-22
申请人： Werner Bonrath , Claus Dittel , Lisa Giraudi , Thomas Netscher , Thomas Pabst
发明人： Werner Bonrath , Claus Dittel , Lisa Giraudi , Thomas Netscher , Thomas Pabst
IPC分类号： C07D311/04
CPC分类号： C07D311/72
摘要： The present invention is concerned with a novel process for the manufacture of α-tocopheryl acetate which comprises reacting 2,3,6-trimethylhydroquinone-1-acetate with a compound selected from the group consisting of phytol (formula IV with R═OH), iso-phytol (formula III with R═OH), and (iso) phytol derivatives represented by the following formulae III and IV with R═C2-to C5-alkonoyloxy, benzoyloxy, mesyloxy, bezenesul-fonyloxy or tosyloxy, (IV) in the presence of a catalyst of the formula Mn+(R1SO3−)n, wherein Mn+ is a silver, copper, gallium, hafnium or rare earth metal cation, n is the valence of the cation Mn+, and R1 is fluorine, C1-8-perfluoroalkyl or perfluoroaryl, and, if required, cyclizing any 3-phytyl-2,5,6-trimethylhydroquinone-1-acetate or a double bond isomer thereof obtained as an intermediate reaction product, to produce α-tocopheryl acetate. In the catalyst Mn+ is preferably Ag+, Cu+, Ga3+, Sc3+, Lu3+, Ho3+, Tm3+, Yb3+ or Hf4+.
摘要翻译：本发明涉及制备乙酸α-生育酚酯的新方法，其包括使2,3,6-三甲基氢醌-1-乙酸酯与选自植醇（式IV与R-OH）的化合物反应，异山嵛醇（具有R-OH的式III）和由下式III和IV表示的（iso）植醇醇衍生物，其具有至少2个至5个C 5 - 烷酰氧基，苯甲酰氧基，甲磺酰氧基，bezenesul-fonyloxy或tosylox

5. 发明授权

US07435836B2 Process for the manufacture of tocopheryl acylates 有权
标题翻译：生产生物基酰基化物的方法
公开(公告)号：US07435836B2
公开(公告)日：2008-10-14
申请号：US11578549
申请日：2005-04-18
申请人： Werner Bonrath , Lisa Giraudi Bijasson
发明人： Werner Bonrath , Lisa Giraudi Bijasson
IPC分类号： C07D311/72
CPC分类号： C07D311/72
摘要： The present invention relates to a process for the manufacture of a tocopheryl acylate which comprises reacting a tocopherol with an acylating agent in the presence of a solid basic catalyst comprising, an alkali metal and/or alkaline earth metal preferably on a solid carrier and to the use of such catalysts in the acylation of tocopherols.
摘要翻译：本发明涉及一种生产生育酚酰化物的方法，其包括在固体碱性催化剂存在下使生育酚与酰化剂反应，所述固体碱性催化剂包含碱金属和/或碱土金属，优选在固体载体上，在酰化生育酚中使用这种催化剂。

6. 发明授权

US07321053B2 Process for the manufacture of tocyl and tocopheryl acylates 有权
标题翻译：制备辛酰基和生育酚酰化物的方法
公开(公告)号：US07321053B2
公开(公告)日：2008-01-22
申请号：US10554885
申请日：2004-04-27
申请人： Werner Bonrath , Lisa Giraudi
发明人： Werner Bonrath , Lisa Giraudi
IPC分类号： C07C67/02
CPC分类号： C07D311/72
摘要： A process for the manufacture of a tocyl acylate or a tocopheryl acylate comprises reacting tocol or a tocopherol with an acylating agent in the presence of a solid heterogeneous Brönsted acid catalyst, said catalyst being an inorganic Brönsted acid on a solid carrier material which comprises silicon dioxide, titanium dioxide or both silicon dioxide and titanium dioxide, or being an organofunctional polysilonaxe featuring sulpho groups, the solid heterogeneous Brönsted acid catalyst further featuring a BET surface area from about 10 m2/g to about 800 m2/g and a pore volume from about 0.1 ml/g to about 2.0 ml/g. The main commercial form of vitamin E, being (all-rac)-α-tocopheryl acetate, can be manufactured by acylation of (all-rac)-α-tocopherol according to this process.
摘要翻译：制备酰基酰化物或生育酚酰基化物的方法包括在固体异质布朗斯台德酸催化剂存在下，将酰基转化成醇或生育酚，所述催化剂是固体载体材料上的无机布朗斯台德酸，其包含二氧化硅，二氧化钛或二氧化硅二氧化钛，或者是具有硫酸基的有机官能聚异氰酸酯，该固体异质布朗斯台德酸催化剂还具有约10m 2 / g至约800μm的BET表面积 2 / g，孔体积为约0.1ml / g至约2.0ml / g。维生素E的主要商业形式是（全脱氧）-α-生育酚乙酸酯，可以通过根据该方法酰化（全 - 外消旋）-α-生育酚来制备。

7. 发明授权

US07105686B2 Manufacture of tocol, tocol derivatives and tocopherols 失效
标题翻译： tocol，tocol衍生物和生育酚的制造
公开(公告)号：US07105686B2
公开(公告)日：2006-09-12
申请号：US10916274
申请日：2004-08-11
申请人： Lisa Giraudi , Werner Bonrath
发明人： Lisa Giraudi , Werner Bonrath
IPC分类号： C07D311/72
CPC分类号： C07D311/72
摘要： The present invention is concerned with a novel process for the manufacture of tocol, tocol derivatives and tocopherols, especially α-tocopherol, by the reaction of a hydroquinone featuring 0 to 3 methyl groups, especially 2,3,5-trimethylhydroquinone, with isophytol, phytol or a(n) (iso)phytol derivative, most preferably with isophytol, in the presence of gadolinium trifluoromethanesulfonate, Gd(OSO2CF3)3, as the catalyst in a biphasic solvent system. This biphasic solvent system consists essentially of a polar organic solvent and a non-polar organic solvent. The polar organic solvent is preferably ethylene carbonate and/or propylene carbonate. The non-polar solvent is preferably at least a solvent selected from the group consisting of hexane, heptane, octane, cyclohexane and methylcyclohexane.
摘要翻译：本发明涉及通过具有0至3个甲基，特别是2,3,5-三甲基对苯二酚的氢醌与异麦芽糖醇的反应制备托卡因，多肽衍生物和生育酚，特别是α-生育酚的新方法， phytol或（n）（iso）phytol衍生物，最优选与异麦芽糖醇混合，在三氟甲磺酸钆存在下，Gd（OSO 2 CF 3）3 / SUB>作为双相溶剂体系中的催化剂。该双相溶剂系统基本上由极性有机溶剂和非极性有机溶剂组成。极性有机溶剂优选为碳酸亚乙酯和/或碳酸亚丙酯。非极性溶剂优选为选自己烷，庚烷，辛烷，环己烷和甲基环己烷中的至少一种溶剂。

8. 发明申请

US20050038269A1 Manufacture of tocol, tocol derivatives and tocopherols 失效
标题翻译： tocol，tocol衍生物和生育酚的制造
公开(公告)号：US20050038269A1
公开(公告)日：2005-02-17
申请号：US10916274
申请日：2004-08-11
申请人： Lisa Giraudi , Werner Bonrath
发明人： Lisa Giraudi , Werner Bonrath
IPC分类号： C07D311/72 , C07D311/74
CPC分类号： C07D311/72
摘要： The present invention is concerned with a novel process for the manufacture of tocol, tocol derivatives and tocopherols, especially α-tocopherol, by the reaction of a hydroquinone featuring 0 to 3 methyl groups, especially 2,3,5-trimethylhydroquinone, with isophytol, phytol or a(n) (iso)phytol derivative, most preferably with isophytol, in the presence of gadolinium trifluoromethanesulfonate, Gd(OSO2CF3)3, as the catalyst in a biphasic solvent system. This biphasic solvent system consists essentially of a polar organic solvent and a non-polar organic solvent. The polar organic solvent is preferably ethylene carbonate and/or propylene carbonate. The non-polar solvent is preferably at least a solvent selected from the group consisting of hexane, heptane, octane, cyclohexane and methylcyclohexane.
摘要翻译：本发明涉及通过具有0至3个甲基，特别是2,3,5-三甲基对苯二酚的氢醌与异麦芽糖醇的反应制备托卡因，多肽衍生物和生育酚，特别是α-生育酚的新方法， phytol或（n）（iso）phytol衍生物，最优选与异麦芽糖醇混合，在三氟甲磺酸钆存在下，Gd（OSO 2 CF 3）3作为双相溶剂体系中的催化剂。该双相溶剂系统基本上由极性有机溶剂和非极性有机溶剂组成。极性有机溶剂优选为碳酸亚乙酯和/或碳酸亚丙酯。非极性溶剂优选为选自己烷，庚烷，辛烷，环己烷和甲基环己烷中的至少一种溶剂。

9. 发明授权

US09108925B2 Process for the manufacture of a precursor of vitamin B1 有权
标题翻译：制造维生素B1前体的方法
公开(公告)号：US09108925B2
公开(公告)日：2015-08-18
申请号：US11795957
申请日：2006-01-24
申请人： Werner Bonrath , Jocelyn Fischesser , Lisa Giraudi , Reinhard Karge
发明人： Werner Bonrath , Jocelyn Fischesser , Lisa Giraudi , Reinhard Karge
IPC分类号： C07D239/42 , C07D239/50 , C07D417/06
CPC分类号： C07D239/42 , C07D417/06
摘要： The present invention relates to a novel process for the manufacture of Grewe-diamine comprising the following step: hydrolyzing a compound of formula (II), wherein R is hydrogen or straight- or branched chain C1-4 alkyl, with an aqueous alkali or alkaline-earth metal hydroxide solution, characterized in that the hydrolysis is carried out in the presence of an organic solvent.
摘要翻译：本发明涉及一种制备Grewe-二胺的新方法，包括以下步骤：将式（II）化合物（其中R是氢或直链或支链C 1-4烷基）与碱或碱水溶液水解 - 碱金属氢氧化物溶液，其特征在于水解是在有机溶剂的存在下进行的。

10. 发明申请

US20070225509A1 Process for the Manufacture of Tocopheryl Acylates 有权
标题翻译：生育酚酸酯的制备方法
公开(公告)号：US20070225509A1
公开(公告)日：2007-09-27
申请号：US11578549
申请日：2005-04-18
申请人： Werner Bonrath , Lisa Giraudi
发明人： Werner Bonrath , Lisa Giraudi
IPC分类号： C07D311/58
CPC分类号： C07D311/72
摘要： The present invention relates to a process for the manufacture of a tocopheryl acylate which comprises reacting a tocopherol with an acylating agent in the presence of a solid basic catalyst comprising, an alkali metal and/or alkaline earth metal preferably on a solid carrier and to the use of such catalysts in the acylation of tocopherols.
摘要翻译：本发明涉及一种生产生育酚酰化物的方法，其包括在固体碱性催化剂存在下使生育酚与酰化剂反应，所述固体碱性催化剂包含碱金属和/或碱土金属，优选在固体载体上，在酰化生育酚中使用这种催化剂。

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