C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/12 (2006.01) C07D 235/28 (2006.01) C07D 413/14 (2006.01) C07D 471/04 (2006.01) C07D 495/04 (2006.01) C07F 3/02 (2006.01)
Patent
CA 2251636
A novel process for the preparation of a magnesium salt of a substituted sulfinyl heterocyclic compound containing an imidazole moiety according to formula I. The process is carried out by mixing the substituted heterocycle of formula (I) with a weak base and a magnesium source. The base and the magnesium source are selected to result in residues, which are easy to remove during the reaction. The invention also relates to the use of the produced compounds in medicine. Compounds according to formula I are: (see formula I) wherein Ar is (see formula II or III) Z is (see formula IV or V) and X is (see formula VI or VII) wherein, N inside the benzene ring of the benzimidazole moiety means that one of the carbon atoms substituted by R7-R10 optionally may be exchanged for a nitrogen atom without any substituents; R1, R2 and R3 are the same or different and are selected from the croup consisting of hydrogen, alkyl, alkylthio, alkoxy, fluorine-substituted alkoxy, alkoxyalkoxy, dialkylamino, piperidino, morpholino, halogen, phenylalkyl and phenylalkoxy, wherein alkyl and alkoxy groups may be branched or linear or contain a cyclic alkyl group; R4 and R5 are the same or different rind are selected from the group consisting of hydrogen, alkyl and aralkyl; R6 is selected from the group consisting of hydrogen, halogen, trifluoromethyl, alkyl and alkoxy; R7-R10 are the same or different and are selected from the group consisting of hydrogen, alkyl, alkoxy, halogen, haloalkoxy, alkylcarbonyl, alkoxycarbonyl, oxazolyl and trifluoroalkyl; R11 is hydrogen; and R12 and R13 are the same of different and are selected from the group consisting of hydrogen, halogen, alkyl and alkoxy groups, wherein alkoxy groups may be branched or straight C1-C9-chains or contain a cyclic alkyl group.
Cette invention concerne un nouveau procédé de préparation d'un sel de magnésium d'un composé hétérocyclique sulfinyle substitué contenant un fragment imidazole, lequel sel de magnésium correspond à la formule générale (I). Ce procédé consiste à mélanger l'hétérocycle substitué correspondant à la formule (I) avec une base faible et avec une source de magnésium. La base et la source de magnésium sont choisis de manière à produire des résidus qui puissent être facilement éliminés lors de la réaction. Cette invention concerne également l'utilisation dans le domaine de la médecine des composés ainsi produits.
Hogberg Jan-Ake
Ioannidis Panagiotis
Mattson Anders
Astra Aktiebolag
Fetherstonhaugh & Co.
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