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    Method for producing substituted biphenyls
    56.
    发明授权
    Method for producing substituted biphenyls 有权
    生产取代联苯的方法

    公开(公告)号：US08461390B2

    公开(公告)日：2013-06-11

    申请号：US13001070

    申请日：2009-06-22

    Applicant: Sebastian Peer Smidt ,  Volker Maywald ,  Kathrin Wissel-Stoll ,  Joachim Schmidt-Leithoff ,  Ansgar Gereon Altenhoff ,  Michael Keil

    Inventor： Sebastian Peer Smidt ,  Volker Maywald ,  Kathrin Wissel-Stoll ,  Joachim Schmidt-Leithoff ,  Ansgar Gereon Altenhoff ,  Michael Keil

    IPC: C07C205/06

    CPC classification number: C07C205/11 ,  C07C201/12

    Abstract: A process for preparing substituted biphenyls of the formula I where R1=nitro or amino, R2=cyano, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy or C1-C4-haloalkylthio, n=from 0 to 3, and R3=hydrogen, cyano or halogen, which comprises reacting a halobenzene of the formula II in which Hal is chlorine or bromine, in the presence of a base and of a palladium catalyst which consists of palladium and a bidentate phosphorus ligand of the formula III where Ar is phenyl which is substituted if desired and R4 and R5 are each C1-C8-alkyl or C3-C6-cycloalkyl or together form a 2- to 7-membered bridge which may, if desired, bear a C1-C6-alkyl substituent, in a solvent or diluent, with a phenylboronic acid IVa a diphenylborinic acid IVb or a mixture of IVa and IVb.

    Abstract translation: 制备式I的取代的联苯的方法，其中R 1 =硝基或氨基，R 2 =氰基，卤素，C 1 -C 4卤代烷基，C 1 -C 4卤代烷氧基或C 1 -C 4卤代烷硫基，n = 0至3， =氢，氰基或卤素，其包括在碱的存在下使Hal为氯或溴的式II的卤代苯与由式III的二齿磷配体组成的钯催化剂反应，其中Ar 是如果需要被取代的苯基，并且R 4和R 5各自是C 1 -C 8 - 烷基或C 3 -C 6 - 环烷基或一起形成2-7元桥，如果需要，其可以具有C 1 -C 6烷基取代基， 在溶剂或稀释剂中与苯基硼酸IVa为二苯基硼酸IVb或IVa和IVb的混合物。

    Anticancer and Tubulin Polymerisation Inhibition Activity of Benzylidene Indanones and Process of Preparing the Same
    57.
    发明申请
    Anticancer and Tubulin Polymerisation Inhibition Activity of Benzylidene Indanones and Process of Preparing the Same 有权
    苯亚甲基内酰胺的抗癌和微管蛋白聚合抑制活性及其制备方法

    公开(公告)号：US20130079396A1

    公开(公告)日：2013-03-28

    申请号：US13623161

    申请日：2012-09-20

    Applicant: Council of Scientific and Industrial Research

    Inventor： Arvind Singh Negi ,  Ayyampudur Palanisamy Prakasham ,  Ajit Kumar Saxena ,  Suaib Luqman ,  Debabrata Chanda ,  Tandeep Kaur ,  Atul Gupta

    IPC: C07C49/755 ,  C07C201/12 ,  C07C45/72 ,  C07D317/54 ,  C07C205/45

    CPC classification number: C07C49/755 ,  C07C45/72 ,  C07C45/74 ,  C07C201/12 ,  C07C205/45 ,  C07C2102/08 ,  C07C2602/08 ,  C07D317/54

    Abstract: The present invention relates to benzylidene indanones of general formula 1. The compounds exhibited tubulin polymerisation inhibition. A series of compounds 2-benzylidene 3-(3,4,5-trimethoxyphenyl) indanones having general formulae 1 were synthesized from gallic acid through a chemical process. 2-(3,4-Methylenedioxybenzylidine), 3-(3,4,5-trimethoxyphenyl), 4,5,6-trimethoxyindanone (8), a representative compound of this series possessing the molecular formulae C29H28O9, was synthesized from gallic acid and exhibits potent anticancer activity. Compound 8 was evaluated for acute oral activity in Swiss albino mice and found to be safe up to 300 mg/kg body weight. The anticancer activity of the compounds has been determined, in order to obtain new potent and cost effective molecules using an in vitro cytotoxicity assay.

    Abstract translation: 本发明涉及通式1的亚苄基茚满酮。该化合物表现出微管蛋白聚合抑制作用。 通过化学方法由没食子酸合成一系列化合物，具有通式1的2-亚苄基3-（3,4,5-三甲氧基苯基）茚满酮。 2-（3,4-亚甲基二氧基亚苄基），3-（3,4,5-三甲氧基苯基），4,5,6-三甲氧基茚满酮（8），具有分子式C29H28O9的该系列的代表性化合物，由没食子酸 并具有很强的抗癌活性。 评估化合物8在瑞士白化病小鼠中的急性口服活性，发现其安全性高达300mg / kg体重。 已经确定了化合物的抗癌活性，以便使用体外细胞毒性测定来获得新的有效和成本有效的分子。

    Alkali metal fluoride dispersion and process for producing fluorine-containing organic compound using the same
    58.
    发明授权
    Alkali metal fluoride dispersion and process for producing fluorine-containing organic compound using the same 失效
    碱金属氟化物分散体及使用其的含氟有机化合物的制造方法

    公开(公告)号：US08399710B2

    公开(公告)日：2013-03-19

    申请号：US12675042

    申请日：2008-08-27

    Applicant: Koji Hagiya

    Inventor： Koji Hagiya

    IPC: C07C45/90

    CPC classification number: C07B39/00 ,  C01D3/02 ,  C07C17/208 ,  C07C51/00 ,  C07C51/58 ,  C07C51/60 ,  C07C67/14 ,  C07C201/12 ,  C07C63/30 ,  C07C69/76 ,  C07C205/12

    Abstract: An alkali metal fluoride dispersion of an alkali metal fluoride and an aprotic organic solvent is obtainable by (A) separating a liquid phase from an alkali metal fluoride dispersion comprising an alcohol solvent and an alkali metal fluoride, and mixing the separated liquid phase with an aprotic organic solvent having a boiling point of 85° C. or higher at normal pressure; (B) obtaining a mixture containing the alkali metal fluoride by (b1) concentrating the mixture containing the alkali metal fluoride to obtain a concentrated fraction and a concentrated residue; (b2) mixing a residue of the alkali metal fluoride dispersion with the concentrated fraction obtained in (b1); and (b3) separating a liquid phase from the mixture containing an alkali metal fluoride obtained in (b2) and mixing the separated liquid phase with the concentrated residue; and (C) removing the alcohol solvent from the mixture containing the alkali metal fluoride.

    Abstract translation: 碱金属氟化物和非质子性有机溶剂的碱金属氟化物分散体可以通过（A）从包含醇溶剂和碱金属氟化物的碱金属氟化物分散液中分离液相，并将分离的液相与非质子 常压下沸点为85℃以上的有机溶剂; （B）通过（b1）浓缩含有碱金属氟化物的混合物得到含有碱金属氟化物的混合物，得到浓缩馏分和浓缩残渣; （b2）将碱金属氟化物分散体的残渣与（b1）中得到的浓缩馏分混合; 和（b3）从含有（b2）中得到的碱金属氟化物的混合物中分离液相并将分离的液相与浓缩残余物混合; 和（C）从含有碱金属氟化物的混合物中除去醇溶剂。

    POTASSIUM FLUORIDE DISPERSION AND PROCESS FOR PRODUCING FLUORINE-CONTAINING ORGANIC COMPOUND USING THE SAME
    59.
    发明申请
    POTASSIUM FLUORIDE DISPERSION AND PROCESS FOR PRODUCING FLUORINE-CONTAINING ORGANIC COMPOUND USING THE SAME 审中-公开
    氟代氟化物分散体及其生产含有氟的有机化合物的方法

    公开(公告)号：US20130060032A1

    公开(公告)日：2013-03-07

    申请号：US13648793

    申请日：2012-10-10

    Applicant: Koji HAGIYA ,  Kazuaki SASAKI

    Inventor： Koji HAGIYA ,  Kazuaki SASAKI

    IPC: C09K3/00 ,  C07C67/14 ,  C07C17/20 ,  C07D239/30 ,  C07C51/58 ,  C07C201/12

    CPC classification number: C07B39/00 ,  C01D3/02 ,  C07C17/208 ,  C07C67/14 ,  C07C201/12 ,  C07C22/08 ,  C07C69/76 ,  C07C205/12

    Abstract: A potassium fluoride dispersion essentially consisting of potassium fluoride and an aprotic organic solvent having a boiling point higher than that of methanol, which is obtainable by mixing a mixture containing potassium fluoride and 5 to 50 parts by weight of methanol per 1 part by weight of potassium fluoride with the aprotic organic solvent followed by concentrating the obtained mixture, and a process for producing a fluorine-containing organic compound comprising contacting an organic compound having at least one group capable of being substituted nucleophilically with a fluorine atom with the potassium fluoride dispersion.

    Abstract translation: 基本上由氟化钾和沸点高于甲醇的非质子有机溶剂组成的氟化钾分散液，其通过将含有氟化钾的混合物和5至50重量份的甲醇混合，每1重量份的钾 用非质子有机溶剂氟化，然后浓缩所得混合物，以及含氟有机化合物的制备方法，包括使具有至少一个能够被氟原子取代的基团的有机化合物与氟原子分散体接触。

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