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    Process for the production of a racemic thioctic acid
    1.
    发明授权
    Process for the production of a racemic thioctic acid 有权
    制备外消旋硫辛酸的方法

    公开(公告)号：US06844450B2

    公开(公告)日：2005-01-18

    申请号：US10398891

    申请日：2001-10-08

    申请人： Annibale Salvi ,  Stefano Maiorana ,  Francesco Corcella

    发明人： Annibale Salvi ,  Stefano Maiorana ,  Francesco Corcella

    IPC分类号： C07D339/04 ,  C07D341/00

    CPC分类号： C07D339/04

    摘要： Process for the synthesis of racemic thioctic acid comprising the following stages: a) reaction of the alkyl ester of 6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis selected from the group consisting of quaternary ammonium or phosphonium salts having the following general formula: where: A is nitrogen of phosphorus, X is selected from the group consisting of Cl, Br, I, HSO4, and H2PO4 and the substitutents R1, R2, R3 and R4 are selection from the group consisting of linear or branched alkyl radicals having one to twenty carbon atoms (C1-C20), said substituents being identical or different one from the other, or only one of said substituents is selected from the group consisting of arylalkyl radicals having the following formula —(CH2)nC6H5 in which n=1-16; b) followed by the hydrolysis of the ester of racemic thiotic acid.

    摘要翻译： 包括以下步骤合成外消旋硫辛酸的方法：a）在相转移化合物存在下，6,8-二卤代辛酸的烷基酯在有机溶剂中与碱性二硫化物水溶液的反应 选自具有以下通式的季铵或鏻盐的催化剂：其中：A是磷的氮，X选自Cl，Br，I，HSO 4和H 2 PO 4，取代基R1，R2 ，R3和R4选自具有1-20个碳原子的直链或支链烷基（C1-C20），所述取代基彼此相同或不同，或者只有一个所述取代基选自基团 由具有下式的芳基烷基 - （CH 2）n C 6 H 5，其中n = 1-16; b）然后水解外消旋硫酸的酯。

    Solid lercanidipine free base
    6.
    发明申请
    Solid lercanidipine free base 审中-公开
    固体氯卡地平游离碱

    公开(公告)号：US20060199849A1

    公开(公告)日：2006-09-07

    申请号：US11364861

    申请日：2006-02-27

    申请人： Fabio Berlati ,  Amedeo Leonardi ,  Gianni Motta ,  Ilaria Candiani ,  Francesco Corcella

    发明人： Fabio Berlati ,  Amedeo Leonardi ,  Gianni Motta ,  Ilaria Candiani ,  Francesco Corcella

    IPC分类号： C07D211/82 ,  A61K31/44

    CPC分类号： C07D211/90

    摘要： The invention provides substantially pure lercanidipine free base, having a purity of at least 95%, preferably at least 97%, more preferably at least 99%, and still more preferably at least 99.5%. The lercanidipine free base of the present invention is formed as an amorphous solid that is easily handled and particularly well suited to the formulation of pharmaceutical compositions.

    摘要翻译： 本发明提供基本上纯的氯卡地平碱，其纯度至少为95％，优选至少97％，更优选至少99％，还更优选至少99.5％。 本发明的氯卡地平游离碱形成为易于处理的非晶态固体，特别适用于药物组合物的制剂。