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38 条记录 (耗时 0.029 秒)

    Process for production of piperidine derivatives
    31.
    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：US06974872B2

    公开(公告)日：2005-12-13

    申请号：US10212854

    申请日：2002-08-05

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

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

    IPC分类号： A61K31/00 ,  A61K31/42 ,  A61K31/421 ,  A61K31/445 ,  A61P37/00 ,  A61P37/08 ,  C07D211/22 ,  C07D211/54 ,  C07D261/04 ,  C07D263/10 ,  C07D211/14 ,  C07D419/10

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

    摘要： The present invention discloses processes for preparing piperidine derivative compounds of the formulae: 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; R 1是氢或羟基; R 2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 > 2 ，条件是当n为1时，R 1和R 2各自为氢; R 3是-COOH或-COOR 4; R 4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
    32.
    发明授权
    Process for production of piperidine derivatives 失效

    公开(公告)号：US06919458B2

    公开(公告)日：2005-07-19

    申请号：US10212829

    申请日：2002-08-05

    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 ,  C07D419/10

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

    摘要： The present invention relates to a process for preparing piperidine derivative compounds of the formulae: 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, The process comprises providing a regiosomer of the following formula: wherein Z is —CG1G2G3, 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 NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; and R5, R8, and R9 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety and converting the regioisomer to the piperidine derivative compound with a piperidine compound.

    Process for production of piperidine derivatives
    33.
    发明授权
    Process for production of piperidine derivatives 有权
    哌啶衍生物的制备方法

    公开(公告)号：US06452011B1

    公开(公告)日：2002-09-17

    申请号：US09634169

    申请日：2000-08-09

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

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

    IPC分类号： C07D21134

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

    摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: where Z is or and where m is 1 or 4-6; Q and Y are the same or different and are selected from the group consisting of O, S, and NR5; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

    摘要翻译： 本发明涉及通过用哌啶化合物转化具有下式的区域异构体来制备哌啶衍生物化合物的方法：其中Z为异或其中m为1或4-6; Q和Y相同或不同，选自O，S和NR5; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R5，R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，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
    34.
    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：US06201124B1

    公开(公告)日：2001-03-13

    申请号：US08575344

    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： C07D21134

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

    摘要： The present invention relates to a method for preparing piperidine derivative compounds by converting, with a piperidine compound, regioisomers having the formula: 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 NR5; G1, G2, and G3 are the same or different and are selected from the group consisting of OR8, SR8, and NR8R9; R6 and R7 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, an aryl moiety, OR8, SR8, and NR8R9; X3 is halogen, OR15, SR15, NR15R16, OSO2R15, or NHSO2R15; R5, R8, R9, R15, and R16 are the same or different and are selected from the group consisting of hydrogen, an alkyl moiety, and an aryl moiety; and A is a substituent of its ring and is selected from the group consisting of hydrogen, halogens, alkyl, hydroxy, alkoxy, and other substituents.

    摘要翻译： 本发明涉及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; R6和R7相同或不同，并且选自氢，烷基部分，芳基部分，OR8，SR8和NR8R9; X3是卤素，OR15，SR15，NR15R16，OSO2R15或NHSO2R15; R5，R8，R9，R15和R16相同或不同，并且选自氢，烷基部分和芳基部分; 并且A是其环的取代基，并且选自氢，卤素，烷基，羟基，烷氧基和其它取代基。

    Piperidine derivatives
    37.
    发明授权
    Piperidine derivatives 失效
    哌啶衍生物

    公开(公告)号：US5578610A

    公开(公告)日：1996-11-26

    申请号：US456273

    申请日：1995-05-31

    申请人： Thomas E. D'Ambra

    发明人： Thomas E. D'Ambra

    IPC分类号： A61K31/00 ,  A61K31/445 ,  A61K31/451 ,  A61K31/4515 ,  A61P11/08 ,  A61P27/00 ,  A61P27/14 ,  A61P37/08 ,  C07C59/84 ,  C07C59/86 ,  C07C59/88 ,  C07C59/90 ,  C07C69/738 ,  C07C69/76 ,  C07D211/20 ,  C07D211/22 ,  C07D211/32 ,  C07D211/70 ,  C07D211/34

    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: ##STR1## wherein R.sub.1 is hydrogen or hydroxy;R.sub.2 is hydrogen;or R.sub.1 and R.sub.2 taken together form a second bond between the carbon atoms bearing R.sub.1 and R.sub.2 ;R.sub.3 is --COOH or --COOR.sub.4 ;R.sub.4 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： 本发明涉及基本上纯的下式的哌啶衍生物化合物：或羟基; R2是氢; 或者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; R3是-COOH或-COOR4; R4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。

    Amine preparation
    38.
    发明授权
    Amine preparation 失效
    胺制剂

    公开(公告)号：US5504253A

    公开(公告)日：1996-04-02

    申请号：US276214

    申请日：1994-07-15

    申请人： Bradford C. VanWagenen ,  Thomas E. D'Ambra

    发明人： Bradford C. VanWagenen ,  Thomas E. D'Ambra

    IPC分类号： C07C213/10 ,  C07C217/58 ,  C07C233/22 ,  C07C209/48 ,  C07C209/50

    CPC分类号： C07C217/58 ,  C07C213/10 ,  C07C233/22

    摘要： A method of making (R)-N- 1-(3-methoxyphenyl)ethyl!-3-(2-chlorobenzene)propanamine which involves reducing the appropriate amidyl or iminyl precursor with an appropriate reducing agent. The appropriate amidyl or iminyl precursor is made from a synthesis involving the use of (R)-3-methoxy-.alpha.-methylbenzylamine. A method of condensing a nitrile with a primary or secondary amine to form an imine involves the reaction of a nitrile with diisobutylaluminum hydride; and then reacting the resultant compound with a primary or secondary amine to form the imine. The process is especially useful for producing enantiomerically pure chiral imines, and, ultimately, amines. Typical such imines have the formula: ##STR1## wherein R, R.sub.1, R.sub.2 and R.sub.3 are independently selected from the group consisting of hydrogen, substituted or unsubstituted alkyl, aryl and aralkyl.

    摘要翻译： 制备（R）-N- [1-（3-甲氧基苯基）乙基] -3-（2-氯苯）丙胺的方法，其涉及用合适的还原剂还原合适的酰胺基或亚氨基前体。 合适的酰氨基或亚氨基前体由涉及使用（R）-3-甲氧基-α-甲基苄胺的合成制备。 将腈与伯胺或仲胺缩合形成亚胺的方法涉及腈与氢化二异丁基铝的反应; 然后使所得化合物与伯胺或仲胺反应形成亚胺。 该方法特别适用于产生对映体纯的手性亚胺，最终产生胺。 典型的这种亚胺具有下式：其中R，R 1，R 2和R 3独立地选自氢，取代或未取代的烷基，芳基和芳烷基。