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    PROCESS FOR THE PRODUCTION OF BENZOFURANS
    85.
    发明申请
    PROCESS FOR THE PRODUCTION OF BENZOFURANS 有权
    生产苯甲醚的方法

    公开(公告)号：US20120065411A1

    公开(公告)日：2012-03-15

    申请号：US13321754

    申请日：2010-05-26

    申请人： Gerhard Kretzschmar ,  Volker Kraft ,  Thomas Olpp ,  Kai Rossen

    发明人： Gerhard Kretzschmar ,  Volker Kraft ,  Thomas Olpp ,  Kai Rossen

    IPC分类号： C07D307/80 ,  C07C205/45 ,  C07C201/12 ,  C07C205/43

    CPC分类号： C07D307/80 ,  C07C205/45

    摘要： A process for the production of 2-alkyl-3-aroyl-5-nitrobenzofurans by acylation of 2-(2-hydroxy-5-nitrophenyl)-1-aryl-ethanones and subsequent treatment of the esters with combinations of bases and proton acids or Lewis acids. This process can be used for the production of Dronedarone. Furthermore, novel intermediates for the manufacture of Dronedarone are provided.

    摘要翻译： 通过2-（2-羟基-5-硝基苯基）-1-芳基乙酰胺的酰化生产2-烷基-3-芳酰基-5-硝基苯并呋喃的方法，随后用碱和质子酸的组合处理酯 或路易斯酸。 该方法可用于生产决奈达隆。 此外，还提供了制备决奈达隆的新型中间体。

    POLYMER ORGANOCATALYST AND PREPARATION PROCESS
    86.
    发明申请
    POLYMER ORGANOCATALYST AND PREPARATION PROCESS 审中-公开
    聚合物有机物和制备方法

    公开(公告)号：US20110034654A1

    公开(公告)日：2011-02-10

    申请号：US12812315

    申请日：2009-01-07

    申请人： Tore Hansen ,  Finn Knut Hansen ,  Tor Erik Kristensen

    发明人： Tore Hansen ,  Finn Knut Hansen ,  Tor Erik Kristensen

    IPC分类号： C08F126/06 ,  C07C205/45

    CPC分类号： C08F26/06

    摘要： A chiral polymer organocatalyst comprising a main chain and side chain organocatalytic groups covalently attached to the main chain, which organocatalytic groups comprise an amino acid or amino acid derivative of the following general formula (I), in which one stereoisomeric form predominates: formula (I) wherein the catalyst is bound to the polymer main chain via R1, R2, R4, R5 or R6 through a linker (L) or direct bond, and wherein R1-R6 and Z are defined as follows: R1 is H, a naturally occurring alpha-amino acid side chain or a non-natural commercially available alpha-amino acid side chain that may contain L; R2 is H, O (doubly bonded to give a carbonyl), O-L (where L is a linker), NH-L or L; R3 is H or doubly bonded to give a carbonyl with R2 when R2 is O; R4 is H, C1-C6 alkyl or L R5 is H, CO2H, C1-C6 alkyl, benzyl, L, CONHR (in which R is alkyl, aryl, heteroaryl, arylalkyl or, heteroarylalkyl), tetrazolyl, CH2 coupled to a triazole moiety, an esterified CH2OH or CO2R (in which R is alkyl, aryl, heteroaryl, arylalkyl N or heteroarylalkyl), formula (II) or formula (III) wherein z is formula (IV) or a directed bond, X4 is H, Me3Si or Et3Si, X3 comprises a naturally-occurring alpha-amino acid side chain, H, C1-C6 alkyl or phenyl, Ar1 and Ar2 are each independently aryl or heteroaryl, and Y denotes the position of attachment to the main chain or linker; and R6 is H, CO2H3 C1-C6 alkyl, benzyl or L; and wherein the polymer organocatalyst comprises a cross-linked polymer.

    摘要翻译： 一种手性聚合物有机催化剂，其包含与主链共价连接的主链和侧链有机催化基团，该有机催化基团包含以下通式（I）的氨基酸或氨基酸衍生物，其中一种立体异构形式占主导地位：式（I ）其中催化剂通过连接基（L）或直接键通过R 1，R 2，R 4，R 5或R 6与聚合物主链结合，并且其中R 1 -R 6和Z定义如下：R 1是H，天然存在的 α-氨基酸侧链或可以含有L的非天然的市售α-氨基酸侧链; R 2是H，O（双键合得到羰基），O-L（其中L是连接基），NH-L或L; 当R 2为O时，R 3为H或双键结合，得到具有R 2的羰基; R4是H，C1-C6烷基或L R5是H，CO2H，C1-C6烷基，苄基，L，CONHR（其中R是烷基，芳基，杂芳基，芳基烷基或杂芳基烷基），四唑基， 部分，酯化的CH 2 OH或CO 2 R（其中R是烷基，芳基，杂芳基，芳基烷基N或杂芳基烷基），式（II）或式（III）其中z是式（IV）或定向键，X 4是H，Me 3 Si 或Et 3 Si，X 3包含天然存在的α-氨基酸侧链，H，C 1 -C 6烷基或苯基，Ar 1和Ar 2各自独立地为芳基或杂芳基，Y表示与主链或连接基连接的位置。 并且R 6是H，CO 2 H 3 C 1 -C 6烷基，苄基或L; 并且其中所述聚合物有机催化剂包含交联聚合物。