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filingDate 1987-06-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f00ee89044a2a11c803aea9902c6325d
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publicationDate 1992-12-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber YU-46054-B
titleOfInvention PROCEDURE FOR OBTAINING IMIDASOCHINOLINE DERIVATIVES
abstract A process for the preparation of imidazoquinoline derivatives of the formula wherein R 1 is halogen, C 1-4 alkyl, C 1-4 alkoxy or trifluoromethyl; R 2 is hydrogen, halogen, C 1-4 alkyl or C 1-4 alkoxy; R 3 is hydrogen, halogen, C 1-4 alkyl or C 1-4 alkoxy; and R 4 is hydrogen or C 1-4 alkyl, and pharmaceutically acceptable salts, hydrates and solvates thereof, which is reduced by a substituted hydantoin of the formula: wherein R 1, R 2, R 3 and R 4 are as defined above and ia and are hydrogen atoms or a covalent bond, by hydrogenation in a solvent such as dimethylformamide, at atmospheric pressure to an overpressure of about 4.2 bar, at room temperature and in the presence of a catalyst such as palladium-on-carbon, to give an intermediate of formula: wherein R1 , R 2, R 3, R 4, a and b have the meanings as defined above, which cyclize to a compound of formula: wherein R 1, R 2, R 3 and R 4 are as defined above, in a solvent such as methanol or ethanol, at the reflux temperature of the reaction mixtures and in the presence of an acid, such as p-toluenesulfonic acid, and the resulting intermediate is subjected to dehydrogenation with iodine, in a solvent such as dimethylformamide and at reflux temperature, to give the desired product of formula (XII); and wherein the compound of formula (XII) is optionally converted into its pharmaceutically acceptable salt and isolated in the form of a hydrate or solvate.
priorityDate 1985-04-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 37.