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    Piperidine derivatives and process for their production
    3.
    发明授权
    Piperidine derivatives and process for their production 失效
    哌啶衍生物及其生产工艺

    公开(公告)号：US07390906B2

    公开(公告)日：2008-06-24

    申请号：US11455531

    申请日：2006-06-19

    申请人： Thomas E. D'Ambra

    发明人： Thomas E. D'Ambra

    IPC分类号： C07D211/22 ,  C07D211/40

    CPC分类号： C07D211/20 ,  C07C59/86 ,  C07C69/738 ,  C07D211/22 ,  C07D211/32

    摘要： The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

    摘要翻译： 本发明涉及下列基本上纯的哌啶衍生物化合物：其中R 1是氢或羟基; R 2是氢; 或R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键， ; R 3是-COOH或-COOR 4; R 4具有1至6个碳原子; A，B和D是它们各自的环的取代基，其各自可以不同或相同，并且是氢，卤素，烷基，羟基，烷氧基或其它取代基。 还公开了以基本上纯的形式制备这种哌啶衍生物化合物的方法。

    Heteroatom functionalized .alpha.-methyl ketones
    4.
    发明授权
    Heteroatom functionalized .alpha.-methyl ketones 失效
    杂原子官能化的α-甲基酮

    公开(公告)号：US5693847A

    公开(公告)日：1997-12-02

    申请号：US424802

    申请日：1995-04-19

    申请人： Roger D. Tung ,  Thomas E. D'Ambra

    发明人： Roger D. Tung ,  Thomas E. D'Ambra

    IPC分类号： C07D303/36

    CPC分类号： C07D303/36

    摘要： The present invention relates to functionalized ketones and novel processes for synthesizing those ketones. The processes of this invention are especially well suited for synthesizing .alpha.-methyl leaving group functionalized ketones. This invention also relates to processes for using .alpha.-methyl leaving group functionalized ketones to produce other compounds and intermediates useful in those processes.

    摘要翻译： 本发明涉及功能化酮和合成这些酮的新方法。 本发明的方法特别适用于合成α-甲基离去基团官能化酮。 本发明还涉及使用α-甲基离去基团官能化酮来生产其它化合物和在这些方法中有用的中间体的方法。

    Process for production of piperidine derivatives
    6.
    发明授权
    Process for production of piperidine derivatives 失效
    哌啶衍生物的制备方法

    公开(公告)号：US07560561B2

    公开(公告)日：2009-07-14

    申请号：US11123275

    申请日：2005-05-06

    申请人： Thomas E. D'Ambra ,  Garry Pilling

    发明人： Thomas E. D'Ambra ,  Garry Pilling

    IPC分类号： C07D211/54

    CPC分类号： C07D211/54 ,  C07D211/22 ,  C07D261/04

    摘要： The present invention discloses processes for preparing piperidine derivative compounds of the formula: wherein n is 0 or 1; R1 is hydrogen or hydroxy; R2 is hydrogen; or, when n is 0, R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2, provided that when n is 1, R1 and R2 are each hydrogen; R3 is —COOH or —COOR4; R4 is an alkyl or aryl moiety; A, B, and D are the substituents of their rings, each of which may be different or the same, and are selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

    摘要翻译： 本发明公开了制备下式的哌啶衍生物化合物的方法：其中n为0或1; R1是氢或羟基; R2是氢; 或者当n为0时，R 1和R 2一起形成带有R 1和R 2的碳原子之间的第二个键，条件是当n为1时，R 1和R 2各自为氢; R3是-COOH或-COOR4; R4是烷基或芳基部分; A，B和D是它们的环的取代基，其各自可以不同或相同，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。

    Process for production of piperidine derivatives
    7.
    发明授权
    Process for production of piperidine derivatives 失效
    哌啶衍生物的制备方法

    公开(公告)号：US6153754A

    公开(公告)日：2000-11-28

    申请号：US576068

    申请日：1995-12-21

    申请人： Thomas E. D'Ambra ,  Garry M. Pilling

    发明人： Thomas E. D'Ambra ,  Garry M. Pilling

    IPC分类号： C07D211/22 ,  A61K31/00 ,  A61K31/42 ,  A61K31/421 ,  A61K31/445 ,  A61P37/00 ,  A61P37/08 ,  C07D211/14 ,  C07D211/34 ,  C07D211/44 ,  C07D211/46 ,  C07D263/10

    CPC分类号： C07D211/22 ,  C07D211/14 ,  C07D211/20 ,  C07D211/46

    摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: ##STR1## where Z is --CG.sup.1 G.sup.2 G.sup.3, ##STR2## and where m is an integer from 1 to 6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR.sup.5 ; G.sup.1, G.sup.2, and G.sup.3 are the same or different and are selected from the group consisting of OR.sup.8, SR.sup.8, and NR.sup.8 R.sup.9 ; and R.sup.5, R.sup.8, and R.sup.9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety.

    摘要翻译： 本发明涉及一种通过用哌啶化合物转化具有下式的区域异构体制备哌啶衍生物化合物的方法：其中Z为-CG1G2G3，m为1至6的整数; Q和Y相同或不同，选自O，S和NR5; G1，G2和G3相同或不同，选自OR8，SR8和NR8R9; 并且R 5，R 8和R 9相同或不同，并且选自氢，烷基部分和芳基部分。

    2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine intermediates
    8.
    发明授权
    2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine intermediates 失效
    2-或3-氨基甲基-4-氨基-3,4-二氢-2H-1,4-苯并恶嗪中间体

    公开(公告)号：US5109135A

    公开(公告)日：1992-04-28

    申请号：US744558

    申请日：1991-08-13

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D265/36 ,  C07D498/06 ,  C07D505/00

    CPC分类号： C07D505/00 ,  C07D265/36

    摘要： 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

    摘要翻译： 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶唑内酯，可用作止痛剂，通过2-或3- 氨基甲基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪与芳基羧酸卤化物在路易斯酸存在下反应，或通过2-或3-氨基甲基-4-氨基 - 3,4-二氢-2H-1,4-苯并恶嗪与1-低级烷基-3-芳基-1,3-二酮或β-二芳基-β-酮戊二醛在脱水条件下反应，加热得到的腙 酸性介质。

    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazin es
    9.
    发明授权
    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazin es 失效
    2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪

    公开(公告)号：US5066803A

    公开(公告)日：1991-11-19

    申请号：US509441

    申请日：1990-04-16

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D265/36 ,  C07D498/06 ,  C07D505/00

    CPC分类号： C07D265/36 ,  C07D505/00

    摘要： 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

    摘要翻译： 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶唑内酯，可用作止痛剂，通过2-或3- 氨基甲基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪与芳基羧酰卤在路易斯酸存在下反应，或通过2-或3-氨基甲基-4-氨基-3 ，4-二氢-2H-1,4-苯并恶嗪与1-低级烷基-3-芳基-1,3-二酮或β-芳基-β-酮戊二醛在脱水条件下反应，并将所得腙加入酸 中。

    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo(1,2,3-DE)-1,4-benzoxazin es
    10.
    发明授权
    2- and 3-aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo(1,2,3-DE)-1,4-benzoxazin es 失效
    2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并（1,2,3-DE）-1,4-苯并恶嗪

    公开(公告)号：US4939138A

    公开(公告)日：1990-07-03

    申请号：US447469

    申请日：1989-12-07

    申请人： Thomas E. D'Ambra ,  Malcolm R. Bell

    发明人： Thomas E. D'Ambra ,  Malcolm R. Bell

    IPC分类号： C07D265/36 ,  C07D498/06 ,  C07D505/00

    CPC分类号： C07D505/00 ,  C07D265/36

    摘要： 2- and 3-Aminomethyl-6-arylcarbonyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazines, useful as analgesic agents, are prepared either by reaction of a 2- or 3-aminomethyl-2,3-dihydropyrrolo[1,2,3-de]-1,4-benzoxazine with an arylcarboxylic acid halide in the presence of a Lewis acid or by reaction of a 2- or 3-aminomethyl-4-amino-3,4-dihydro-2H-1,4-benzoxazine with a 1-lower-alkyl-3-aryl-1,3-diketone or with a .beta.-aryl-.beta.-ketopropionaldehyde under dehydrating conditions and heating the resulting hydrazone in an acid medium.

    摘要翻译： 2-和3-氨基甲基-6-芳基羰基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶唑内酯，可用作止痛剂，通过2-或3- 氨基甲基-2,3-二氢吡咯并[1,2,3-de] -1,4-苯并恶嗪与芳基羧酸卤化物在路易斯酸存在下反应，或通过2-或3-氨基甲基-4-氨基 - 3,4-二氢-2H-1,4-苯并恶嗪与1-低级烷基-3-芳基-1,3-二酮或β-二芳基-β-酮戊二醛在脱水条件下反应，加热得到的腙 酸性介质。