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    Manufacture of tocopheryl acetate
    1.
    发明申请
    Manufacture of tocopheryl acetate 审中-公开
    醋酸生育酚的制造

    公开(公告)号：US20070112206A1

    公开(公告)日：2007-05-17

    申请号：US11639029

    申请日：2006-12-13

    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： C07D311/02

    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-trimethylhydro-quinone-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-3-enyl]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 产生生育酚乙酸酯的闭环反应。 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-3-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。

    Bag dispenser
    2.
    发明授权
    Bag dispenser 失效
    袋装机

    公开(公告)号：US5325992A

    公开(公告)日：1994-07-05

    申请号：US092945

    申请日：1993-07-19

    申请人： Josef Koller ,  Rudolf Schmid

    发明人： Josef Koller ,  Rudolf Schmid

    IPC分类号： B65B67/12 ,  A47F13/08 ,  A47K10/38 ,  B65B61/12 ,  B65D83/08 ,  B65H35/00 ,  B65H1/00

    CPC分类号： B65H35/008 ,  A47F13/085 ,  A47K10/3827 ,  B65B61/12 ,  A47F2009/044 ,  Y10T225/393

    摘要： A dispensing device including a container for a supply of items forming a web. The dispensing device includes a recess formed in an outer wall of the container, a braking unit overlapping the recess. The braking unit includes two lips which work together when items are dispensed and a linear slit between the two lips which enables the items to pass between the two lips, the two lips being fitted with bristles which constitute active elements of the two lips, unattached ends of the bristles of one of the lips extend into, and mesh with, an area of unattached ends of the bristles of the opposite lip. The items are camisole-shaped and sequentially joined bags having a body with a bottom part and handles at the upper part. The bottom part of the body of one of the bags is connected to the leading edge of the handles of the next bag. A nozzle for dispensing the bags is connected to the recess, the nozzle including a hollow cover in the base of which there is an oblong and virtually linear opening, the distance between the edges of the opening being considerably larger than the thickness of a bag. The braking unit is attached to the hollow cover in such a way that it overlaps the linear opening in the hollow cover.

    摘要翻译： PCT No.PCT / CH91 / 00031 Sec。 371 1991年12月10日第 102（e）日期1991年12月10日PCT 1991年2月7日提交PCT公布。 公开号WO91 / 11942 日期1991年8月22日。一种分配装置，包括用于供应形成网的物品的容器。 分配装置包括形成在容器的外壁中的凹部，与凹部重叠的制动单元。 制动单元包括两个嘴唇，当物品被分配时一起工作，并且两个嘴唇之间的线性狭缝使得物品能够在两个嘴唇之间通过，两个唇部装配有构成两个嘴唇的有源元件的刷毛，未附着的端部 其中一个嘴唇的刷毛延伸到相对唇缘的刷毛的未附着端部的区域中并与其啮合。 这些物品是具有底部的主体和上部的手柄的吊带形状和顺序连接的袋。 其中一个袋子的主体的底部连接到下一个袋子的把手的前缘。 用于分配袋子的喷嘴连接到凹部，喷嘴包括在其基部中的中空盖，其具有长方形和实质上线性的开口，开口边缘之间的距离远大于袋的厚度。 制动单元以与中空盖中的线性开口重叠的方式附接到中空盖。

    Process for the Preparation of Pyrido [2,1-a] Isoquinoline Derivatives by Catalytic Asymmetric Hydrogenation of an Enamine
    4.
    发明申请
    Process for the Preparation of Pyrido [2,1-a] Isoquinoline Derivatives by Catalytic Asymmetric Hydrogenation of an Enamine 审中-公开
    通过胺的催化不对称氢化制备吡啶并[2,1-a]异喹啉衍生物的方法

    公开(公告)号：US20120010413A1

    公开(公告)日：2012-01-12

    申请号：US13235766

    申请日：2011-09-19

    申请人： Stefan Abrecht ,  Michelangelo Scalone ,  Rudolf Schmid

    发明人： Stefan Abrecht ,  Michelangelo Scalone ,  Rudolf Schmid

    IPC分类号： C07D455/08

    CPC分类号： C07D455/06 ,  B01J31/2295 ,  B01J2231/641 ,  B01J2531/822 ,  C07D471/04 ,  Y02P20/55

    摘要： The invention relates to a process for the preparation of pyrido[2,1-a] isoquinoline derivatives of the formula wherein R2, R3 and R4 are as defined in the specification, comprising the steps of a) catalytic asymmetric hydrogenation of an enamine of the formula wherein R1 is lower alkyl, in the presence of a transition metal catalyst containing a chiral diphosphane ligand, b) introduction of an amino protecting group Prot and c) amidation of the ester to form an amide of formula wherein R2, R3, R4 and Prot are as defined in the specification.

    摘要翻译： 本发明涉及制备下式吡啶并[2,1-a]异喹啉衍生物的方法，其中R2，R3和R4如说明书中所定义，包括以下步骤：a）催化不对称氢化 式中R 1是低级烷基，在含有手性二膦配体的过渡金属催化剂的存在下，b）引入氨基保护基团Prot和c）酰胺化该酯以形成下式的酰胺，其中R2，R3，R4和 Prot如规范中所定义。

    Chiral amido-phosphine-phosphinite compounds
    5.
    发明授权
    Chiral amido-phosphine-phosphinite compounds 失效
    手性酰胺 - 膦 - 磷化合物

    公开(公告)号：US06348612B1

    公开(公告)日：2002-02-19

    申请号：US09035554

    申请日：1998-03-05

    申请人： Wolfgang Burkart ,  Michelangelo Scalone ,  Rudolf Schmid

    发明人： Wolfgang Burkart ,  Michelangelo Scalone ,  Rudolf Schmid

    IPC分类号： C07F9141

    CPC分类号： C07F15/008 ,  B01J31/188 ,  B01J2231/645 ,  B01J2531/80 ,  B01J2531/821 ,  B01J2531/822 ,  B01J2531/824 ,  B01J2531/827 ,  C07B53/00 ,  C07F9/46 ,  C07F9/65515 ,  C07F9/6568 ,  C07F15/004 ,  C07F15/0053 ,  C07F15/0066

    摘要： Novel chiral amidophosphine-phosphinite compounds, which are present in (R) and (S) form, of the general formula wherein R1 signifies alkyl, cycloalkyl or aralkyl, R2 signifies alkyl, cycloalkyl, aralkyl or aryl and R3 and R4 each independently signify alkyl, cycloalkyl, aralkyl, aryl or heteroaryl or R3 and R4 together with the respective phosphorus atom signify a 9-dibenzophospholyl, 9-phosphabicyclo[3.3.1]nonyl or 9-phosphabicyclo[4.2.1]nonyl group and * denotes a chiral center, are manufactured by reacting a compound of the general formula R1C(OH)—CONHR2 (III) with a disubstituted chlorophosphane of the general formula R3R4PCl (IV) in a solvent and in the presence of a base. As ligands the amidophosphine-phosphinite compounds in accordance with the invention form complexes with Group VIII transition metals, especially with rhodium, iridium, ruthenium and palladium, and optionally with further ligands, and such complexes are likewise an object of the present invention; they can be used as catalysts for enantioselective reactions, especially for asymmetric hydrogenations, enantioselective hydrogen displacements and allylic substitution reactions.

    摘要翻译： 通式（R）和（S）中存在的新型手性酰氨基膦 - 膦酸盐化合物表示烷基，环烷基或芳烷基，R2表示烷基，环烷基，芳烷基或芳基，R3和R4各自独立地表示烷基， 环烷基，芳烷基，芳基或杂芳基或R 3和R 4与各自的磷原子一起表示9-二苯并磷杂，9-磷杂双环[3.3.1]壬基或9-磷杂双环[4.2.1]壬基，*表示手性中心， 通过使通式R 1 C（OH）-CONHR 2（III）的化合物与通式R 3 R 4 PCl（IV）的二取代氯代膦在溶剂中和碱的存在下反应制备。 作为配体，根据本发明的酰胺膦 - 膦系化合物与第Ⅷ族过渡金属形成络合物，特别是与铑，铱，钌和钯以及任选的其它配体形成络合物，并且这种络合物同样是本发明的目的; 它们可以用作对映选择性反应的催化剂，特别是用于不对称氢化，对映选择性氢位移和烯丙基取代反应。

    Racemization of atropisomeric bis(phosphine oxide) compounds
    6.
    发明授权
    Racemization of atropisomeric bis(phosphine oxide) compounds 有权
    无规异构双（氧化膦）化合物的外消旋化

    公开(公告)号：US06288280B1

    公开(公告)日：2001-09-11

    申请号：US09594643

    申请日：2000-06-15

    申请人： Frank Kienzle ,  Michel Lalonde ,  Rudolf Schmid ,  Shaoning Wang

    发明人： Frank Kienzle ,  Michel Lalonde ,  Rudolf Schmid ,  Shaoning Wang

    IPC分类号： C07F953

    CPC分类号： C07F9/5329 ,  C07F9/5054

    摘要： A process for the racemization of atropisomeric bis(phosphine oxide) compounds of formula I: in their (S) or (R) or non-racemic form, is useful for preparing optical active bisphosphine ligands, that form optical active complexes with transition metals. Racemization is thermal and carried out in high or low boiling solvent, under normal or elevated pressure at 105 to 3.5×107 Pa. Heating is performed in a system that allows heating up to 400° C. (reactor, autoclave, aluminum block, round-bottom flask with heating/stirring mantle and the like) or by microwave irradiation or in the melt at a temperature from 260 to 400° C.

    摘要翻译： 式（I）或（R）或非外消旋形式的式I的阻转异构双（氧化膦）化合物外消旋化的方法可用于制备与过渡金属形成光学活性配合物的光学活性双膦配体。 外消旋化是热和在高沸点溶剂或低沸点溶剂中，在正常或升高的压力下，在105-3.5×10 7 Pa下进行，在允许加热到400℃的系统中进行加热（反应器，高压釜，铝块， 具有加热/搅拌罩等的底烧瓶）或通过微波照射或在260-400℃的温度下在熔体中进行。

    Breakaway hinge for eyeglasses
    7.
    发明授权
    Breakaway hinge for eyeglasses 失效
    眼镜折角铰链

    公开(公告)号：US5980039A

    公开(公告)日：1999-11-09

    申请号：US83254

    申请日：1998-05-20

    申请人： Rudolf Schmid ,  Wilhelm Anger

    发明人： Rudolf Schmid ,  Wilhelm Anger

    IPC分类号： F16C11/04 ,  G02C1/02 ,  G02C5/00 ,  G02C5/14 ,  G02C5/22

    CPC分类号： B29C45/0046 ,  G02C1/02 ,  G02C5/006 ,  G02C5/10 ,  G02C5/2209 ,  B29L2012/005 ,  B29L2031/22 ,  G02C2200/04 ,  Y10T16/526

    摘要： A hinge for glasses pivotably connects an endpiece (2) attached directly on a lens (3) or provided on a frame with a temple (1). The hinge has a hinge pin (12) held rotatably in a hinge support (22) of the endpiece (2), which hinge pin is disposed on the temple (1). The hinge pin (12) forms a predetermined breaking point (122) for the hinge, which releases the temple (1) when an admissible force on the endpiece (2) is exceeded. A preferred embodiment is described, according to which the hinge pin (12) is formed in one piece with the temple (1) in an injection molding process.

    摘要翻译： 用于眼镜的铰链将直接附接在透镜（3）上或设置在框架上的端部件（2）可枢转地连接到镜腿（1）。 铰链具有可旋转地保持在端件（2）的铰链支撑件（22）中的铰链销（12），该铰链销设置在镜腿（1）上。 铰链销（12）形成用于铰链的预定断裂点（122），当超过端部件（2）上的允许力时，释放凸起（1）。 描述了优选实施例，根据该优选实施例，铰链销（12）在注射成型工艺中与镜腿（1）成一体地形成。