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    Formation of N-protected bis-3,6-(4-aminoalkyl)-2,5,diketopiperazine
    4.
    发明授权
    Formation of N-protected bis-3,6-(4-aminoalkyl)-2,5,diketopiperazine 有权
    形成N-保护的双-3,6-（4-氨基烷基）-2,5，二酮哌嗪

    公开(公告)号：US08912328B2

    公开(公告)日：2014-12-16

    申请号：US13368172

    申请日：2012-02-07

    申请人： John J. Freeman ,  Adrienne Stamper ,  Melissa Heitmann

    发明人： John J. Freeman ,  Adrienne Stamper ,  Melissa Heitmann

    IPC分类号： C07D241/06 ,  C07D241/08 ,  B01J31/02

    CPC分类号： C07D241/08 ,  B01J31/0225 ,  B01J31/0258 ,  B01J31/0259 ,  B01J2231/40

    摘要： The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1-propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.

    摘要翻译： 所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。 特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-（氨基烷基）-2,5-二酮哌嗪的改进方法。 公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法，包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。 催化剂选自硫酸，磷酸，对甲苯磺酸，1-丙基膦酸环状酸酐，磷酸三丁酯，苯基膦酸和五氧化二磷等。 溶剂选自二甲基乙酰胺，N-甲基-2-吡咯烷酮，二甘醇二甲醚，甘醇二甲醚，丙二醇，乙基二甘醇二甲醚，间甲酚，对甲酚，邻甲酚，二甲苯，乙二醇和苯酚等。

    Compound
    7.
    发明申请
    Compound 有权
    复合

    公开(公告)号：US20040019016A1

    公开(公告)日：2004-01-29

    申请号：US10300494

    申请日：2002-11-20

    发明人： Barry Victor Lloyd Potter ,  Lok Wai Lawrence Woo ,  Atul Purohit ,  Michael John Reed ,  Oliver Brook Sutcliffe ,  Christian Bubert

    IPC分类号： A61K031/495 ,  A61K031/445 ,  A61K031/18 ,  C07F005/02 ,  C07D241/06 ,  C07C311/10

    CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D413/12 ,  C07D417/12

    摘要： There is provided a compound of Formula I 1 wherein each T is independently selected from H, hydrocarbyl, nullFnullR, and a bond with one of D, E, P or Q, or together with one of P and Q forms a ring; Z is a suitable atom the valency of which is m; D, E and F are each independently of each other an optional linker group, wherein when Z is nitrogen E is other than CH2 and CnullO; P, Q and R are independently of each other a ring system; and at least Q comprises a sulphamate group.

    摘要翻译： 提供式I的化合物，其中每个T独立地选自H，烃基，-F-R和与D，E，P或Q之一的键，或与P和Q中的一个形成环; Z是一个合适的原子，其化合价是m; D，E和F各自独立地为任选的连接基团，其中当Z为氮时，E不是CH 2且C = O; P，Q和R彼此独立地是环系; 并且至少Q包含氨基磺酸酯基团。