Process for the preparation of 9-amino camptothecin
    6.
    发明授权
    Process for the preparation of 9-amino camptothecin 失效
    制备9-氨基喜树碱的方法

    公开(公告)号:US06403603B1

    公开(公告)日:2002-06-11

    申请号:US08284129

    申请日:1994-08-02

    IPC分类号: C07D49122

    CPC分类号: C07D491/22

    摘要: 9-Amino-20(S)-camptothecin (I) is prepared by reducing 12-nitro-20(S)-camptothecin (II); converting the resulting 12-amino-20(S)-camptothecin (III) into a compound of formula (IV) wherein X is a group which can be reductively removed; reacting the compound of formula (IV) with a nitrating agent, to obtain thereby the corresponding 9-nitro-20(S)-camptothecin compound of formula (V) substituted at the 12-position by the group X; reducing in a single step the compound of formula (V), so obtaining the 9-amino-20(S)-camptothecin of formula (I); or reducing the compound of formula (V), so obtaining the corresponding 9-amino-20(S)-camptothecin compound of formula (VI) substituted at the 12-position by the group X and reductively removing the X group from the compound of formula (VI), so obtaining 9-amino-20(S)-camptothecin.

    摘要翻译: 通过还原12-硝基-20(S) - 喜树碱(II)制备9-氨基-20(S) - 喜树碱(I) 将所得的12-氨基-20(S) - 喜树碱(III)转化成式(IV)的化合物,其中X是可被还原去除的基团; 使式(Ⅳ)化合物与硝化剂反应,由此获得在X-12位被12位取代的相应的9-硝基-20(S)喜树碱化合物。 在一步中还原式(Ⅴ)化合物,从而得到式(I)的9-氨基-20(S) - 喜树碱; 或降低式(Ⅴ)化合物,从而得到在X基上被12位取代的相应的式(Ⅵ)的9-氨基-20(S) - 喜树碱化合物,并将X基团从 式(VI),因此得到9-氨基-20(S) - 喜树碱。

    Process for the preparation and purification of valgancyclovir hydrochloride
    8.
    发明授权
    Process for the preparation and purification of valgancyclovir hydrochloride 有权
    盐酸伐昔洛韦的制备和纯化方法

    公开(公告)号:US07935818B2

    公开(公告)日:2011-05-03

    申请号:US11820724

    申请日:2007-06-20

    IPC分类号: C07D473/18

    CPC分类号: C07D473/18

    摘要: A process for the preparation of valgancyclovir which comprises: a) reacting a compound of formula 7, in an aprotic solvent, in the presence of a condensing agent, with a compound of formula 8, wherein R1, and R2 may be, each independently, hydrogen, an halogen atom or an hydroxyl group; the double bond may either be in the E or Z configuration or a mixture thereof to yield a compound of formula 9 b) mild hydrolysis of compound obtained in a) to give valgancyclovir.

    摘要翻译: 制备valgancyclovir的方法,其包括:a)使式7的化合物在非质子溶剂中在缩合剂存在下与式8的化合物反应,其中R 1和R 2可以各自独立地为氢, 氢,卤素原子或羟基; 双键可以是E或Z构型或其混合物,得到式9的化合物b)在a)中获得的化合物的温和水解得到valgancyclovir。

    ATOMOXETINE HYDROCHLORIDE PURE CRYSTALLINE FORM

    公开(公告)号:US20090156863A1

    公开(公告)日:2009-06-18

    申请号:US12097150

    申请日:2006-11-17

    IPC分类号: C07C217/48

    CPC分类号: C07C217/48 C07C213/10

    摘要: The present invention discloses a process for the preparation of atomoxetine hydrochloride in a pure crystalline form, characterised by an XRPD spectrum as in FIG. 1. It is also object of the present invention to provide methods to obtain pure atomoxetine hydrochloride without the use of methylene chloride.

    摘要翻译: 本发明公开了一种以纯晶体形式制备盐酸阿托西汀的方法,其特征在于如图1所示的XRPD光谱。 本发明的另一个目的是提供在不使用二氯甲烷的情况下获得纯盐酸阿托西汀的方法。