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    Process for the production of r(+)&agr;-lipoic acid
    5.
    发明授权
    Process for the production of r(+)&agr;-lipoic acid 有权
    生产r（+）α-硫辛酸的方法

    公开(公告)号：US06670484B2

    公开(公告)日：2003-12-30

    申请号：US10398892

    申请日：2003-04-09

    申请人： Flavio Villani ,  Antonio Nardi ,  Annibale Salvi ,  Giovanna Falabella

    发明人： Flavio Villani ,  Antonio Nardi ,  Annibale Salvi ,  Giovanna Falabella

    IPC分类号： C07D33902

    CPC分类号： C07D339/04 ,  C07C319/06 ,  C07C323/60

    摘要： Process for the synthesis of R(+)&agr;-lipoic acid comprising the following stages: a) Salifying of racemic thioctic acid with R(+)&agr;-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)&agr;-lipoic acid-R(+)&agr;-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+) &agr;-lipoic acid-R(+)&agr;-methylbenzylamine, in which the re-crystallization solvent consists of a mixture of non-polar/polar solvents; d) separation of the diastereoisomeric salt to obtain R(+)&agr;-lipoic acid by reaction of said salt with acids selected from the group consisting of aliphatic hydroxy-carboxylic acids having 3 to 6 carbon atoms and aqueous phosphoric acid.

    摘要翻译： 包括以下阶段的R（+）α-硫辛酸的合成方法：a）用R（+） - α-甲基苄胺磺化外消旋硫辛酸; b）通过过滤R（+）α-硫辛酸-R（+）α-甲基苄胺的结晶非对映异构体盐分离; c）通过R（+）α-硫辛酸-R（+）α-甲基苄胺的非对映异构体盐的重结晶进行纯化，其中重结晶溶剂由非极性/极性溶剂的混合物组成; d）通过所述盐与选自具有3至6个碳原子的脂肪族羟基羧酸和磷酸水溶液的酸反应，分离非对映异构盐以获得R（+）α-硫辛酸。

    Synthesis of r(+)α-lipoic acid
    8.
    发明授权
    Synthesis of r(+)α-lipoic acid 有权
    r（+）α-硫辛酸的合成

    公开(公告)号：US06864374B2

    公开(公告)日：2005-03-08

    申请号：US10398890

    申请日：2001-10-08

    申请人： Flavio Villani ,  Antonio Nardi ,  Annibale Salvi ,  Giovanna Falabella

    发明人： Flavio Villani ,  Antonio Nardi ,  Annibale Salvi ,  Giovanna Falabella

    IPC分类号： C07B53/00 ,  C07B57/00 ,  C07B61/00 ,  C07C51/41 ,  C07C51/487 ,  C07C53/19 ,  C07C67/08 ,  C07C69/63 ,  C07D339/04 ,  C07D339/02

    CPC分类号： C07D339/04

    摘要： Process for the synthesis of R(+)α-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(−)α-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(−)α-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(−)α-methylbenzylamine; (d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)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; g) hydolysis of the ester of R(+)α-lipoic acid.

    摘要翻译： 包括以下步骤的合成R（+）α-硫辛酸的方法：a）用S（ - ） - α-甲基苄胺磺化外消旋6,8-辛酸; b）通过过滤R（+）6,8-二卤代辛酸-S（ - ）α-甲基苄胺的结晶非对映异构体盐分离; c）通过R（+）6,8-二 - 卤代 - 辛酸-S（ - ） - α-甲基苄胺的非对映异构体盐的重结晶进行纯化; （d）通过用强无机酸在稀释在2至10重量％之间的水溶液中重复所述盐，分离非对映异构盐以获得R（+）6,8-二卤代辛酸; e）R（+）6,8-二卤代辛酸酯化得到相应的烷基酯; f）在相转移催化化合物存在下，R（+）6,8-二卤代辛酸烷基酯在有机溶剂中与碱性二硫化物水溶液的反应; g）R（+）α-硫辛酸的酯的水解。