http://rdf.ncbi.nlm.nih.gov/pubchem/patent/YU-46054-B
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_42e94091a4fc81b8d0237117707cc7ee |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P7-02 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P7-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4745 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
filingDate | 1987-06-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f00ee89044a2a11c803aea9902c6325d http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cb33adc5d528d45b9e0812b35caa6689 |
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 |
Incoming Links
Total number of triples: 37.