公开(公告)号：CA2468437A1

公开(公告)日：2003-06-12

申请号：CA2468437

申请日：2002-12-05

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS

IPC: C07B53/00 ,  C07B61/00 ,  C07C67/31 ,  C07C69/675 ,  C07D339/04

Abstract: The invention relates to a method for the production of dihydroxycarboxylate esters and a total synthesis for the production of R-(+)-.alpha. lipoic acid .

公开(公告)号：DE59902779D1

公开(公告)日：2002-10-24

申请号：DE59902779

申请日：1999-07-12

Applicant: BASF AG

Inventor： KLATT JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM ,  RIEGER JENS

IPC: A23L1/30 ,  A61K31/385 ,  C07B57/00 ,  C07D339/04

Abstract: In the 2 &THgr; diffractogram of an enantiomerically pure crystalline (R)- or (S)-lipoic acid, the most intense reflection line in the range from 13° to 30° is that at 2 &THgr;=23°.

公开(公告)号：AU2957602A

公开(公告)日：2002-06-11

申请号：AU2957602

申请日：2001-11-29

Applicant: BASF AG

Inventor： KLATT MARTIN 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.

公开(公告)号：AU9167701A

公开(公告)日：2002-02-13

申请号：AU9167701

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.

公开(公告)号：DE19834608A1

公开(公告)日：2000-02-03

申请号：DE19834608

申请日：1998-07-31

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM ,  RIEGER JENS

IPC: A23L1/30 ,  A61K31/385 ,  C07B57/00 ,  C07D339/04

Abstract: The invention relates to enantiomer-free crystalline (R) or (S) lipoic acid, where the reflection line at 2 THETA = 23 DEG is the most intensive one in the 13 DEG to 30 DEG range in the 2 THETA diffractogram.

公开(公告)号：ES2266299T3

公开(公告)日：2007-03-01

申请号：ES01990455

申请日：2001-11-29

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM

IPC: C07D339/04

Abstract: Procedimiento para la obtención del ácido R- o S- dihidrolipoico, que comprende (a) la reacción de o sus estereoisómeros, donde MS significan SO2-R¿ y R y R¿ significan, independientemente entre sí, alquilo con 1 a 6 átomos de carbono, cicloalquilo con 3 a 8 átomos de carbono, cicloalquilalquilo con 3 a 8 átomos de carbono, arilo o aralquilo, con sulfuro de sodio y azufre en metanol.

公开(公告)号：CA2417842A1

公开(公告)日：2003-01-30

申请号：CA2417842

申请日：2001-07-24

Applicant: BASF AG

Inventor： PAUST JOACHIM ,  KLATT MARTIN JOCHEN ,  NIEBEL MARKUS

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

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.

公开(公告)号：AU751485B2

公开(公告)日：2002-08-15

申请号：AU4909499

申请日：1999-07-12

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM ,  RIEGER JENS

IPC: A23L1/30 ,  A61K31/385 ,  C07B57/00 ,  C07D339/04

Abstract: In the 2 &THgr; diffractogram of an enantiomerically pure crystalline (R)- or (S)-lipoic acid, the most intense reflection line in the range from 13° to 30° is that at 2 &THgr;=23°.

公开(公告)号：CA2430073A1

公开(公告)日：2002-06-06

申请号：CA2430073

申请日：2001-11-29

Applicant: BASF AG

Inventor： NIEBEL MARKUS ,  KLATT MARTIN JOCHEN ,  PAUST JOACHIM

IPC: 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 SO2R', 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.

公开(公告)号：BR9912622A

公开(公告)日：2001-04-24

申请号：BR9912622

申请日：1999-07-12

Applicant: BASF AG

Inventor： KLATT MARTIN JOCHEN ,  NIEBEL MARKUS ,  PAUST JOACHIM ,  RIEGER JENS

IPC: A23L1/30 ,  A61K31/385 ,  C07B57/00 ,  C07D339/04

Abstract: In the 2 &THgr; diffractogram of an enantiomerically pure crystalline (R)- or (S)-lipoic acid, the most intense reflection line in the range from 13° to 30° is that at 2 &THgr;=23°.