Process for the preparation of sulphoximines

C - Chemistry – Metallurgy – 07 – D

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C07D 209/34 (2006.01) A61K 31/47 (2006.01) C07D 215/22 (2006.01) C07D 401/12 (2006.01) A61K 31/40 (2006.01)

Patent

CA 1201123

Abstract The present invention describes a process for the preparation of sulphoximines of general formula Image (I) wherein A represents a methylene, vinylene or ethylene group (optionally substituted by one or two alyl groups each containing 1 to 3 carbon atoms); B represents a straight-chain or branched alkylene group containing 2 to 6 carbon atoms and R1 represents an alkyl group containing 1 to 3 carbon atoms (optionally substituted by a phenyl group) or a phenyl group (wherein the aforementioned phenyl nuclei may optionally be substituted by an alkyl group con- taining 1 to 4 carbon atoms, by a halogen atom, by an alkoxy group containing 1 to 3 carbon atoms, or by a cyclohexyl, phenyl or halophenyl group); an alkyl group containing 4 to 7 carbon atoms; a cycloalkyl group containing 3 to 7 carbon atoms; a phenyl group di- or tri-substituted by alkyl groups containing 1 to 4 carbon atoms or by alkoxy groups containing 1 to 3 carbon atoms and/or by halogen atoms or a hydroxy- or amino-phenyl group disubstituted by alkyl groups containing 1 to 4 carbon atoms or by alkoxy groups containing 1 to 3 carbon atoms and/or by halogen atoms, wherein the substituents of the abovementioned phenyl, hydroxyphenyl or aminophenyl nuclei may be identi- cal or different; a naphthyl group (optionally substituted by an alkoxy group containing 1 to 3 carbon atoms); or a pyridyl group, which com- prises splitting off an acyl residue from a compound of general formula Image wherein A, B and R1 are defined as hereinbefore and R represents a hydrolytic cleavable acyl residue, by means of hydrolysis. The compounds of the general formula I show valuable pharmacological properties, moreover antithrombotic effects.

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