利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

106 条记录 (耗时 0.025 秒)

    Process for the preparation of Sitagliptin
    37.
    发明授权
    Process for the preparation of Sitagliptin 失效
    西他列汀的制备方法

    公开(公告)号：US08097724B2

    公开(公告)日：2012-01-17

    申请号：US12727566

    申请日：2010-03-19

    申请人： Pietro Allegrini ,  Emanuele Attolino ,  Gianmaria Dell'Anna ,  Mario Michieletti

    发明人： Pietro Allegrini ,  Emanuele Attolino ,  Gianmaria Dell'Anna ,  Mario Michieletti

    IPC分类号： C07D491/00

    CPC分类号： C07D487/04

    摘要： A process for the preparation of a compound of formula (I) such as 2(R)-4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]-7(8H)-pyrazinyl]-1-(2,4,5-trifluorophenyl)-2-butanamine, or a salt thereof, in the anhydrous or hydrated form, either as a mixture of enantiomers, or as a single (R) or (S) enantiomer, comprising the conversion of a compound of formula (II), or a salt thereof, either as a single (R) or (S) enantiomer or as a mixture thereof wherein X is hydrogen, hydroxy, C1-C8 alkyl, C1-C4 alkoxy, aryl, amino, N3 or halogen; into a compound of formula (I), and if desired, the separation of a single enantiomer of formula (I) from the racemic mixture, and/or, if desired, the conversion of a compound of formula (I) into a salt thereof, or vice versa.

    摘要翻译： 制备式（I）化合物如2（R）-4-氧代-4- [3-（三氟甲基）-5,6-二氢[1,2,4]三唑并[4,3 -a] -7（8H） - 吡嗪基] -1-（2,4,5-三氟苯基）-2-丁胺或其盐以无水或水合的形式，作为对映异构体的混合物，或作为 包括将式（II）化合物或其盐转化成单一（R）或（S）对映异构体或其混合物，其中X为氢，羟基 C 1 -C 8烷基，C 1 -C 4烷氧基，芳基，氨基，N 3或卤素; （I）化合物，如果需要，将式（I）的单一对映体与外消旋混合物分离，和/或如果需要，将式（I）化合物转化为其盐 ， 或相反亦然。