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    METHOD FOR PRODUCING DIHYDROXYCARBOXYLIC ESTER IN ABSENCE OF SOLVENT
    1.
    发明专利
    METHOD FOR PRODUCING DIHYDROXYCARBOXYLIC ESTER IN ABSENCE OF SOLVENT 审中-公开

    公开(公告)号：JP2003192638A

    公开(公告)日：2003-07-09

    申请号：JP2002351365

    申请日：2002-12-03

    Applicant: BASF AG

    Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  ERHARDT MELANIE

    IPC: C07D339/04 ,  C07C67/30 ,  C07C67/31 ,  C07C67/317 ,  C07C67/32 ,  C07C69/66 ,  C07C69/675

    Abstract: PROBLEM TO BE SOLVED: To provide a method for producing a dihydroxycarboxylic ester of formula I as an intermediate for producing R-(+)-α-lipoic acid with a relative amount of complex hydrides in the absence of solvent in a high yield. SOLUTION: This method for producing the dihydroxycarboxylic ester represented by formula I [(n) is 1, 2, 3, 4, 5, 6 or 7; R 1 is a substituted or unsubstituted 1 to 20C alkyl, 2 to 20C alkenyl, 2 to 20C alkynyl or the like] comprises reacting a hydroxycarboxylic diester represented by formula II (R 2 is selected from R 1 independently from R 1 ) with the complex hydrides in the absence of solvent. COPYRIGHT: (C)2003,JPO

    METHOD FOR PRODUCING LIPOIC ACID AND DIHYDROLIPOIC ACID
    2.
    发明申请
    METHOD FOR PRODUCING LIPOIC ACID AND DIHYDROLIPOIC ACID 审中-公开
    用于生产硫辛酸和二氢

    公开(公告)号：WO0210151A2

    公开(公告)日：2002-02-07

    申请号：PCT/EP0108523

    申请日：2001-07-24

    Applicant: BASF AG ,  KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

    Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

    IPC: A61K31/20 ,  A61P3/10 ,  C07B53/00 ,  C07C303/38 ,  C07C309/66 ,  C07C319/08 ,  C07C319/18 ,  C07C319/28 ,  C07C321/04 ,  C07C323/52 ,  C07D339/04 ,  C07D339/00

    CPC classification number: C07D339/04 ,  C07C319/18 ,  C07C321/04 ,  C07C323/52

    Abstract: The invention relates to a method for producing R-lipoic acid and S-lipoic acid comprising a step selected from the following: (a) distillation of dihydrolipoic acid, (b) reaction of (2) or the stereoisomer thereof, wherein Ms represents SO2-R', and R and R' independently mean C1-C6-alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkylalkyl, aryl or aralkyl, with sodium sulphide and sulphur in ethanol and reaction with a complex hydride, (c) extraction of a protic solution of R dihydrolipoic acid or S-dihydrolipoic acid with an organic solvent at a pH value of 9 -10, or (d) extraction of R-dihydrolipoic acid or S-dihydrolipoic acid with an organic solvent from a protic solution at a pH value of 4 - 5, or a combination of individual or several steps (a) - (d). The invention also relates to a method for producing dihydrolipoic acid and the compound 1,6,8 octane triol.

    Abstract translation: 为R-α-硫辛酸或S-硫辛酸的制剂，其包含选自（a）的二氢硫辛酸的蒸馏中选择的工艺步骤中，（b）中的反应或它的立体异构体，其中Ms“和R和R”是-SO 2 R独立地C 1 -C过程 C6烷基，C3-C8环烷基，C3-C8-环烷基烷基，芳基或芳烷基，与硫化钠和硫在乙醇中，用复合氢化物的反应中，（c）中R-二氢硫辛酸或S的质子溶液的提取 二氢硫辛酸与有机溶剂在pH值为9〜10，或（d）R-二氢硫辛酸或与来自一个的质子溶液或以4的pH值至5的有机溶剂S-二氢硫辛酸，或它们的组合的提取 更多的步骤（a）至（d）以及方法二氢硫辛酸的制备和化合物1,6,8 Oktantriol。

    METHOD FOR PRODUCING LIPOIC ACID AND DIHYDROLIPOIC ACID
    3.
    发明申请
    METHOD FOR PRODUCING LIPOIC ACID AND DIHYDROLIPOIC ACID 审中-公开
    用于生产硫辛酸和DIHYDROLIPONSAÜRE

    公开(公告)号：WO0244163A3

    公开(公告)日：2003-01-30

    申请号：PCT/EP0113955

    申请日：2001-11-29

    Applicant: BASF AG ,  KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

    Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

    IPC: C07D339/04

    CPC classification number: C07D339/04

    Abstract: The invention relates to a method for producing R- and S-lipoic acid and R-dihydrolipoic acid comprising the following steps: (a) reaction of the compound of formula (2) with sodium sulphide and sulphur in methanol, whereby Ms represents SO R`, and R and R` independently of one another represent C1-C6 alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkylalkyl, aryl or aralkyl. The invention relates in particular to methods for producing pure R- or S-dihydrolipoic acid, which is either used directly or processed further to obtain R- and S-lipoic acid. The method is also used to produce medicaments. The invention also relates to a solution of sodium sulphide-trihydrate and sulphur in methanol, whereby the sulphur is present as a molar surplus in relation to the sodium sulphide-trihydrate, and to a kit that comprises the inventive solution.

    Abstract translation: 本发明涉及一种方法，用于R-和S-硫辛酸和R-二氢硫辛酸的制备，其包括（a）使（I），其中MS是SO <2> R`和R和R`独立地为C1-C6烷基 ，C3-C8环烷基，C3-C8-环烷基烷基，芳基或芳烷基，与硫化钠和硫在甲醇中。 具体而言，本发明提供用于制备纯的R或S-二氢硫辛酸的，其直接或R-和S-硫辛酸涉及进一步的处理中使用的方法。 该方法也可用于制备药物。 本发明还涉及硫化酸钠三水合物和硫的甲醇溶液中，硫是存在的摩尔过量于Natriumsfulfid三水合物和包含本发明的

    4.
    发明专利
    未知

    公开(公告)号：DK1339705T3

    公开(公告)日：2006-10-09

    申请号：DK01990455

    申请日：2001-11-29

    Applicant: BASF AG

    Inventor： KLATT MARTIN JOCHEN ,  PAUST JOACHIM ,  NIEBEL MARKUS

    IPC: C07D339/04

    Abstract: The present invention relates to a process for the preparation of R- and S-lipoic acid and R- and S-dihydrolipoic acid comprising (a) reaction of where MS is SO 2 -R' and R and R' independently of one another are C 1 -C 6 -alkyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkylalkyl, aryl or aralkyl, with sodium sulfide and sulfur in methanol. The invention especially relates to processes for preparing pure R- or S-dihydrolipoic acid, which is either used directly or processed further to give R- and S-lipoic acid. The process also serves for the production of pharmaceuticals. The present invention further relates to a solution of sodium sulfide trihydrate and sulfur in methanol, the sulfur being present in a molar excess over the sodium sulfide trihydrate, and a kit which comprises the solution according to the invention.

    5.
    发明专利
    未知

    公开(公告)号：BR0112848A

    公开(公告)日：2003-06-24

    申请号：BR0112848

    申请日：2001-07-24

    Applicant: BASF AG

    Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

    IPC: A61K31/20 ,  A61P3/10 ,  C07B53/00 ,  C07C303/38 ,  C07C309/66 ,  C07C319/08 ,  C07C319/18 ,  C07C319/28 ,  C07C321/04 ,  C07C323/52 ,  C07D339/04 ,  C07D339/00

    Abstract: Processes for the preparation of R-lipoic acid or S-lipoic acid comprising a process step selected from a) distillation of dihydrolipoic acid, b) reaction of or its stereoisomer, where Ms is SO 2 -R' and R and R' independently of one another is [sic] C 1 -C 6 -alkyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkylalkyl, aryl or aralkyl, with sodium sulfide and sulfur in ethanol and reaction with a complex hydride, (c) the extraction of a protic solution of R-dihydrolipoic acid or S-dihydrolipoic acid with organic solvents at a pH from 9 to 10, or (d) the extraction of R-dihydrolipoic acid or S-dihydrolipoic acid with organic solvents from a protic solution at a pH of 4 to 5, or a combination of one or more of steps (a) to (d), and processes for the preparation of dihydrolipoic acid and the compound 1,6,8 [lacuna] octanetriol.

    10.
    发明专利
    未知

    公开(公告)号：DE50110077D1

    公开(公告)日：2006-07-20

    申请号：DE50110077

    申请日：2001-11-29

    Applicant: BASF AG

    Inventor： KLATT JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

    IPC: C07D339/04

    Abstract: The present invention relates to a process for the preparation of R- and S-lipoic acid and R- and S-dihydrolipoic acid comprising (a) reaction of where MS is SO 2 -R' and R and R' independently of one another are C 1 -C 6 -alkyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkylalkyl, aryl or aralkyl, with sodium sulfide and sulfur in methanol. The invention especially relates to processes for preparing pure R- or S-dihydrolipoic acid, which is either used directly or processed further to give R- and S-lipoic acid. The process also serves for the production of pharmaceuticals. The present invention further relates to a solution of sodium sulfide trihydrate and sulfur in methanol, the sulfur being present in a molar excess over the sodium sulfide trihydrate, and a kit which comprises the solution according to the invention.

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