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    Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11β-hydroxy steroid dehydrogenase type 1
    2.
    发明授权
    Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11β-hydroxy steroid dehydrogenase type 1 失效
    制备1型11β-羟基类固醇脱氢酶的C-5-取代的杂环抑制剂的催化方法

    公开(公告)号：US07541474B2

    公开(公告)日：2009-06-02

    申请号：US11590922

    申请日：2006-11-01

    申请人： Emilio Bunel ,  Anil Guram ,  Qingyian Liu

    发明人： Emilio Bunel ,  Anil Guram ,  Qingyian Liu

    IPC分类号： C07D277/08 ,  C07D263/08

    CPC分类号： C07D277/54 ,  C07D277/42

    摘要： The invention provides a process for preparing 11 β-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

    摘要翻译： 本发明提供了一种在碱存在下通过式1化合物与式R2LG化合物之间的催化反应制备式II的11-羟基类固醇脱氢酶1型抑制剂的方法：其中R1，R2，X，Y， 和LG在说明书中描述。 示例性催化剂含有钯和一种或多种膦配体。 该方法可以以立体选择性方式进行，得到对映异构体富集的产物。

    Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11beta-hydroxy steroid dehydrogenase type 1
    4.
    发明申请
    Catalyzed process of making C-5-substituted heterocyclic inhibitors of 11beta-hydroxy steroid dehydrogenase type 1 失效
    制备1型11β-羟基类固醇脱氢酶的C-5-取代的杂环抑制剂的催化方法

    公开(公告)号：US20070117985A1

    公开(公告)日：2007-05-24

    申请号：US11590922

    申请日：2006-11-01

    申请人： Emilio Bunel ,  Anil Guram ,  Qingyian Liu

    发明人： Emilio Bunel ,  Anil Guram ,  Qingyian Liu

    IPC分类号： C07D263/00 ,  C07D233/80 ,  C07D233/38

    CPC分类号： C07D277/54 ,  C07D277/42

    摘要： The invention provides a process for preparing 11 β-hydroxy steroid dehydrogenase type 1 inhibitors of formula 2 via a catalyzed reaction between a compound of formula 1 and a compound of formula R2LG in the presence of base: where R1, R2, X, Y, and LG are described in the specification. Exemplary catalysts contain palladium and one or more phosphine ligands. The process can be performed in a stereoselective manner to give enantiomerically enriched products.

    摘要翻译： 本发明提供了在碱存在下通过式1化合物与式R 2 LG化合物之间的催化反应来制备式II的11β-羟基类固醇脱氢酶1型抑制剂的方法： 其中R 1，R 2，X，Y和LG在说明书中描述。 示例性催化剂含有钯和一种或多种膦配体。 该方法可以以立体选择性方式进行，得到对映异构体富集的产物。

    Process for making 5-cyanovaleric acid, adipic acid or dimethyl adipate
    5.
    发明申请
    Process for making 5-cyanovaleric acid, adipic acid or dimethyl adipate 失效
    制备5-氰基戊酸，己二酸或己二酸二甲酯的方法

    公开(公告)号：US20060258876A1

    公开(公告)日：2006-11-16

    申请号：US11488197

    申请日：2006-07-17

    申请人： Emilio Bunel ,  David Clark

    发明人： Emilio Bunel ,  David Clark

    IPC分类号： C07C51/15 ,  C07C253/12

    CPC分类号： C07C253/30 ,  C07C51/14 ,  C07C67/38 ,  C07C55/14 ,  C07C69/44 ,  C07C255/19

    摘要： Disclosed in a process for making (1) a compound of the formula NC—CH2—CH2—CH2—CH2—CO2R′, wherein R′ is H or C1 to C12 alkyl, or (2) adipic acid or (3) dimethyl adipate, using as the substrate, 3-pentenenitrile, (2) 3-pentenoic acid or methyl 3-pentenoate, respectively, by contacting the substrate with carbon monoxide and a nucleophile in the presence of a Group VIII metal, a selected ligand, and an acid promoter. The nucleophile, which (a) an alcohol or water, or (b) water or (c) methanol, respectively, in the presence of a Group VIII metal, preferably palladium, a selected phosphine ligand, and an acid promoter.

    摘要翻译： 公开在制备（1）式NC-CH 2 -CH 2 -CH 2 -CH 2的化合物的方法中， 2，其中R'是H或C 1至C 12烷基，或（2）己二酸 酸或（3）己二酸二甲酯，分别使用3-戊烯腈，（2）3-戊烯酸或3-戊烯酸甲酯，通过在第VIII族金属存在下使底物与一氧化碳和亲核试剂接触 ，选择的配体和酸启动子。 在第VIII族金属，优选钯，选择的膦配体和酸促进剂的存在下，分别为（a）醇或水，或（b）水或（c）甲醇）的亲核试剂。