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filingDate 1995-07-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2001-07-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber IL-114477-A
titleOfInvention A process for the enantioselective synthesis of converted sulfoxides, individual enantiomers obtained as a result of the process and their use in the preparation of drugs
abstract A process for enantioselective synthesis of a sulphoxide compound of formula (I) or an alkaline salt thereof either as a single enantiomer or in an enatiomerically enriched form 1607 ד' באב התשס" א - July 24, 2001 wherein Het1 is Het2 is and X is wherein N inside the benzene ring of the benzimidazole moiety means that one of the carbon atoms subsituted by R6-R9 optionally may be exchanged for a nitrogen atom without any substituents; R1, R2 and R3 are the same or different and selected from hydrogen, alkyl, alkylthio, alkoxy optionally substituted by fluorine, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenylalkyl and phenylakoxy; R4 and R5 are the same or different and selected from hydrogen, alkyl and aralkyl; R6 is hydrogen, halogen, trifluoromethyl, alkyl and alkoxy; R6-R9 are the same or different and selected from hydrogen, alkyl, alkoxy, halogen, halo-alkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolyl, trifluoroalkyl, or adjacent groups R6-R9 form ring structures which may be further subtituted; R10 is hydrogen or forms an alkylene chain together with R3; R11 and R12 are the same of different and selected from hydrogen, halogen or alkyl and alkyl groups, alkoxy groups and moieties thereof may be branched or straight C1-C9-chains or comprise cylic alkyl groups, for example cycloalkylalkyl characterized in that a pro-chiral sulphide of the formula Het1 X S Het2 1608 ד' באב התשס" א - July 24, 2001 wherein Het1, and Het2 are as defined above, is oxidised in an organic solvent with an oxidising agent and in the presence of a chiral titanium IV complex and a base, and the obtained sulphoxide optionally is converted into a pharmaceutically acceptable salt by conventional processes. Claimed as novel are (+)-5-methoxy-2-{{(4-methoxy-3, 5-dimethyl-2-pyridinyl) - methyl] sulphinyl]- 1H-benzimidazole and (-)-5-methoxy-2-[[(4-methoxy-3, 5-dimethyl-2-pyridinyl) - methyl] sulphinyl]- 1H-benzimidazole or a pharmaceutically acceptable salt thereof produced by the process claimed.
priorityDate 1994-07-15-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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