http://rdf.ncbi.nlm.nih.gov/pubchem/patent/IE-36016-L
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-80 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-85 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-80 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-85 |
| filingDate | 1971-11-19-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1972-05-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | IE-36016-L |
| titleOfInvention | Nicotinic acid derivatives. |
| abstract | 1317239 2-Hydroxy-nicotinic acids F HOFFMANN-LA ROCHE & CO AG 23 Nov 1971 [23 Nov 1970 (2)] 54366/71 Heading C2C Novel 2-hydroxy-nicotinic acids of the general formula wherein R is a halogen atom in the 5- or 6- position, an amino group in the 4-position or a C 1-4 alkyl group in the 4- or 5-position, and base addition salts thereof are prepared (a) by base hydrolysis of a 2,6-dihalo-nicotinic acid at reflux temperature and acidification of the hydrolysis mixture to give a 6-halo-2-hydroxy-nicotinic acid, (b) by hydrogenation of 2-hydroxy-4- nitro-nicotinic acid-N-oxide to give 4-amino-2- hydroxy-nicotinic acid, (c) by reaction of 4- chloro-2-hydroxy-nicotinic acid with ammonia to give the product of (b), (d) by treatment of 4-chloro-2-hydroxy-nicotinic acid with a C 1-4 alkyl lithium or C 1-4 alkyl magnesium bromide to give a 2-hydroxy-4-C 1-4 alkyl-nicotinic acid, (e) by treatment of a 2-amino-4-C 1-4 alkylnicotinic acid with sodium nitrite and sulphuric acid to give a 2-hydroxy-4-C 1-4 alkyl-nicotinic acid, (f) by treatment of a 2-hydroxy-3-bromo- 5-C 1-4 alkyl-pyridine in an inert solvent with n-butyl lithium and carbon dioxide to give a 2 - hydroxy - 5 - C 1-4 alkyl - nicotinic acid, (g) by acid hydrolysis of a 2-hydroxy-3-cyano-5- C 1-4 alkyl-pyridine to give a 2-hydroxy-5-C 1-4 alkyl-nicotinic acid and (h) by treatment of 2- hydroxy-5-amino-nicotinic acid with sodium nitrite and hydrochloric acid/cuprous chloride or hydrobromic acid/cuprous bromide to give 5 - chloro- or bromo - 2 - hydroxy - nicotinic acid, followed optionally by salification of the product. 2 - Hydroxy - 3 - cyano - 5 - methyl - pyridine is prepared by reaction of 2-amino-3-bromo-5- 5-methyl-pyridine with cuprous cyanide and treatment of the resulting 2-amino-3-cyano-5- methyl-pyridine with sodium nitrite and sulphuric acid. 2 - Amino - 4 - methyl - nicotinic acid is prepared by reaction of 4-methylquinolinic acid with ammonia and reaction of the resulting 3 - carboxy - 4 - methyl - pyridine-2- carboxylic acid amide with aqueous sodium hydroxide and bromine, followed by sulphur dioxide. Pharmaceutical compositions having hypolipidemic activity comprise, as active ingredient, a 2-hydroxy-nicotinic acid of the above general formula or a pharmaceutically acceptable base addition salt thereof, in association with a compatible pharmaceutical carrier.n[GB1317239A] |
| priorityDate | 1970-11-23-04:00^^<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: 65.