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1. WO1996002535 - PROCESS FOR SYNTHESIS OF SUBSTITUTED SULPHOXIDES

Publication Number WO/1996/002535
Publication Date 01.02.1996
International Application No. PCT/SE1995/000818
International Filing Date 03.07.1995
Chapter 2 Demand Filed 07.02.1996
IPC
C07D 235/28 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
24with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
28Sulfur atoms
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
CPC
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
C07D 235/28
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
235Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02condensed with carbocyclic rings or ring systems
04Benzimidazoles; Hydrogenated benzimidazoles
24with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
28Sulfur atoms
C07D 401/12
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
Applicants
  • ASTRA AKTIEBOLAG [SE/SE]; S-151 85 Södertälje, SE (AllExceptUS)
  • LARSSON, Erik, Magnus [SE/SE]; SE (UsOnly)
  • STENHEDE, Urban, Jan [SE/SE]; SE (UsOnly)
  • SÖRENSEN, Henrik [DK/SE]; SE (UsOnly)
  • VON UNGE, Per, Oskar, Sverker [SE/SE]; SE (UsOnly)
  • COTTON, Hanna, Kristina [SE/SE]; SE (UsOnly)
Inventors
  • LARSSON, Erik, Magnus; SE
  • STENHEDE, Urban, Jan; SE
  • SÖRENSEN, Henrik; SE
  • VON UNGE, Per, Oskar, Sverker; SE
  • COTTON, Hanna, Kristina; SE
Agents
  • ASTRA AKTIEBOLAG; Patent Dept. S-151 85 Södertälje, SE
  • LARSSON, Birgitta; ASTRA Aktiebolag S-151 85 Södertalje, SE
Priority Data
9402510-315.07.1994SE
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR SYNTHESIS OF SUBSTITUTED SULPHOXIDES
(FR) PROCEDE DE SYNTHESE DE SULFOXYDES SUBSTITUES
Abstract
(EN)
A novel process for enantioselective synthesis of single enantiomers of omeprazole or its alkaline salts, of other optically pure substituted 2-(2-pyridinylmethyl-sulphinyl)-1H-benzimidazoles as well as of other structurally related sulphoxides or their alkaline salts. The claimed process is an asymmetric oxidation of a pro-chiral sulphide to the single enantiomers or an enantiomerically enriched form of the corresponding sulphoxide. The application also claims the enantiomeric sulphoxide products produced by the process and their use in medicine.
(FR)
La présente invention concerne un nouveau procédé de synthèse énantiosélective d'énantiomères simples d'oméprazole ou de ses sels alcalins, d'autres 2-(2-pyridinylméthyl-sulfinyl)-1H-benzimidazoles substitués, optiquement purs, ainsi que d'autres sulfoxydes structurellement apparentés ou de leurs sels alcalins. Le procédé de la présente invention consiste en une oxydation asymétrique de sulfures pro-chiraux donnant des énantiomères simples ou une forme énantiomériquement enrichie du sulfoxyde correspondant. L'invention concerne également des sulfoxydes énantiomères produits grâce à ce nouveau procédé et leur utilisation en médecine.
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