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33 条记录 (耗时 0.014 秒)

    PROCESS FOR THE PREPARATION OF [2-((8,9)- DIOXO-2,6-DIAZABICYCLO [5.2.0]-NON-1(7)-EN-2-YL)-ETHYL] PHOSPHONIC ACID
    2.
    发明授权
    PROCESS FOR THE PREPARATION OF [2-((8,9)- DIOXO-2,6-DIAZABICYCLO [5.2.0]-NON-1(7)-EN-2-YL)-ETHYL] PHOSPHONIC ACID 失效
    用于生产[2 - （（（8,9-二氧代-2,6-二氮杂双环[5.2.0]壬-1 7） - 烯-2-基）乙基]膦

    公开(公告)号：EP1000072B1

    公开(公告)日：2003-02-19

    申请号：EP98937292.5

    申请日：1998-07-31

    申请人： Wyeth

    发明人： ASSELIN, Andre, Alfred ,  KINNEY, William, Alvin ,  SCHMID, Jean

    IPC分类号： C07F9/645 ,  C07F9/40

    CPC分类号： C07F9/645 ,  C07F9/4006

    摘要： This invention relates to a process for the preparation of formula (I) compound [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid, an NMDA antagonist useful as an anticonvulsant and neuroprotectant in situations involving excess release of excitatory amino acids. In the process of the present invention, 3-aminopropyl carbamic acid 1,1-dimethyl-ethyl ester is reacted with a dialkyl vinylphosphonate to obtain N-[3-(t-butyloxycarbonyl-amino)propyl]-2-aminoethylphosphonic acid dialkyl ester (d) in 80 % yield. Reaction of (d) with a 3,4-dialkoxycyclobut-3-en-1,2-dione gives [3-[[2-(dialkoxyphosphoryl)ethyl]-(2-alkoxy-3,4-dioxo-1,2-cyclobuten-1-yl)amino]propyl] carbamic acid 1,1-dimethylethyl ester (e) in 96 % yield. Deprotection and cyclization of (e) in trifluoroacetic acid gives [2-((8,9)-dioxo-2,6-diazabicyclo[5.2.0]-non-1(7)-en-2-yl)ethyl]phosphonic acid dialkyl ester (c) in 58 % yield. The phosphonic acid diethyl ester (c) was treated with bromotrimethylsilane to give compound (I).

    Amino acid-derived cyclic phosphonamides and methods of synthesizing the same
    4.
    发明公开
    Amino acid-derived cyclic phosphonamides and methods of synthesizing the same 有权
    氨基酸衍生的环状膦酰胺及其合成方法

    公开(公告)号：EP1806351A3

    公开(公告)日：2007-09-26

    申请号：EP07008428.0

    申请日：2001-08-06

    申请人： THE UNIVERSITY OF KANSAS

    发明人： Hanson, Paul R. ,  Sprott, Kevin T. ,  McReynolds, Matthew D.

    IPC分类号： C07F9/22 ,  C07F9/36 ,  C07F9/572 ,  C07F9/645

    CPC分类号： C07F9/2462 ,  C07F9/26 ,  C07F9/6584 ,  C07F9/65842 ,  C07F9/65848

    摘要： New phosphonamide compounds and methods of forming those compounds are provided. In one embodiment, the inventive methods comprise subjecting an opened-ring phosphonamide template to a ring-closing metathesis reaction in the presence of a ring-closing catalyst (e.g., a Grubbs catalyst) to yield a phosphonamide. In another embodiment, the inventive methods comprise reacting a template structure with a phosphorous (III) compound to yield the phosphonamide. Advantageously, in either embodiment, the template structures can be provided with a wide array of functional groups (e.g., amino acid side chains, peptides) chosen to provide particular properties to the compound.

    摘要翻译： 提供了新的膦酰胺化合物和形成这些化合物的方法。 在一个实施方案中，本发明的方法包括使开环膦酰胺模板在闭环催化剂（例如Grubbs催化剂）存在下进行闭环复分解反应以产生膦酰胺。 在另一个实施方案中，本发明的方法包括使模板结构与磷（III）化合物反应以产生膦酰胺。 有利的是，在任一实施方案中，可以为模板结构提供广泛的官能团（例如，氨基酸侧链，肽），所述官能团被选择以向化合物提供特定的性质。

    DERIVATIVES OF [2-(8,9-DIOXO-2,6-DIAZABICYCLO[5.2.0]NON-1(7)-EN-2-YL)ALKYL]PHOSPHONIC ACID AND METHOD OF MAKING THEM
    5.
    发明公开
    DERIVATIVES OF [2-(8,9-DIOXO-2,6-DIAZABICYCLO[5.2.0]NON-1(7)-EN-2-YL)ALKYL]PHOSPHONIC ACID AND METHOD OF MAKING THEM 有权
    导数的[2-（8,9-二氧代-2,6-二氮杂双环[5.2.0]壬-1（7） - 烯-2-基）烷基]用于制造膦AND METHOD

    公开(公告)号：EP1797104A1

    公开(公告)日：2007-06-20

    申请号：EP05803939.7

    申请日：2005-10-06

    申请人： Wyeth

    发明人： BAUDY, Reinhardt, Richard

    IPC分类号： C07F9/645 ,  A61K31/675 ,  A61P25/02

    CPC分类号： A61K31/551 ,  C07F9/645

    摘要： Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided (Formula I): wherein: A is alkylenyl of 1 to 4 carbon atoms, or alkenylenyl of 2 to 4 carbon atoms; R1 and R2 are, independently, hydrogen or a C5 to C7 aryl optionally substituted with 1 to 2 substituents, independently, selected from the group consisting of -C(O)R3, halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy, with the proviso that at least one of R1, and R2 is not hydrogen; R3 is, independently, hydrogen, -OR4, alkyl, aryl, or heteroaryl; R4 is hydrogen, alkyl, aryl, or heteroaryl; R5 and R6 are, independently, hydrogen, alkyl, hydroxyl, alkoxy, or C5 to C7 aryl; wherein any R3 to R6 group having an aryl or heteroaryl moiety can optionally be substituted on the aryl or heteroaryl moiety with 1 to about 5 substituents, independently, selected from the group consisting of halogen, cyano, nitro, hydroxyl, C1-C6 alkyl, and C1-C6 alkoxy. Methods of making these compounds as well as methods using the compounds for treating a variety of conditions are also disclosed.