PROCESS FOR THE PREPARATION OF LINAGLIPTIN
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF LINAGLIPTIN 审中-公开
    制备LINAGLIPTIN的方法

    公开(公告)号:US20120165525A1

    公开(公告)日:2012-06-28

    申请号:US13325179

    申请日:2011-12-14

    IPC分类号: C07D473/04

    CPC分类号: C07D473/04

    摘要: The present invention relates to processes for the preparation of 8-(3R)-3-aminopiperidinyl)-7-butyn-2-yl-3 -methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione and novel intermediates useful in its synthesis.

    摘要翻译: 本发明涉及制备8-(3R)-3-氨基哌啶基)-7-丁炔-2-基-3-甲基-1-(4-甲基 - 喹唑啉-2-基甲基)-3,7 - 二氢嘌呤-2,6-二酮及其合成中有用的新型中间体。

    PROCESS FOR THE PREPARATION OF VARENICLINE
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF VARENICLINE 审中-公开
    制备VARENICLINE的方法

    公开(公告)号:US20130030179A1

    公开(公告)日:2013-01-31

    申请号:US13557340

    申请日:2012-07-25

    IPC分类号: C07D487/08

    CPC分类号: C07D471/08

    摘要: It is disclosed a process for the preparation of a compound of formula (I) or a salt thereof, comprising: nitrating a compound of formula (II) or a salt thereof, to obtain a compound of formula (IV) or a salt thereof, reducing it, to obtain a compound of formula (V) or a salt thereof, and subsequently cyclizing it to obtain a compound of formula (I) or a salt thereof and, if desired, converting a compound of formula (I) to a salt thereof, or vice versa, characterized in that: the nitration of a compound of formula (II) or a salt thereof is carried out with concentrated nitric acid in the presence of a strong inorganic acid and that the amino group in the compound of formula (II) is not protected.

    摘要翻译: 公开了制备式(I)化合物或其盐的方法,其包括:硝化式(II)化合物或其盐,得到式(IV)化合物或其盐, 得到式(Ⅴ)化合物或其盐,然后使其环化得到式(I)化合物或其盐,如果需要,将式(I)化合物转化为盐 其特征在于:式(II)化合物或其盐的硝化在强无机酸存在下用浓硝酸进行,并且式(II)化合物中的氨基 II)没有保护。