http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1451936-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3e9445e5e3626f36e932c6451a928250 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C247-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 |
| filingDate | 1973-12-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1976-10-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1451936-A |
| titleOfInvention | Diazepin derivatives and process for the manufacture thereof |
| abstract | 1451936 Triazolobenzodiazepines CIBAGEIGY AG 12 Dec 1973 [29 Dec 1972] 57584/73 Heading C2C Compounds of the general formula (R 1 = H, C 1-7 alkyl which may be substituted by an optionally etherified or esterified hydroxyl group or by an amino group which is optionally mono- or disubstituted, CHO, COOH, CN, di-(C 1-7 alkoxy)methyl, C 2-8 alkoxycarbonyl, optionally mono- or disubstituted carbamoyl; rings B, C optionally carry one or more substituents selected from F, Cl, Br, CF 3 , NO 2 , C 1-7 alkyl and alkoxy), their 5-oxides and acid addition salts are prepared by (a) condensing a compound of the formula with R 1 <SP>1</SP>C # CCH 2 NH 2 (R 1 <SP>1</SP> = R 1 except esterified hydroxyalkyl, CHO, COOH, alkoxycarbonyl), optionally followed by esterification of a resulting alcohol, oxidation of CH 2 OH to CHO or COOH and conversion of the latter groups to alkoxycarbonyl or carbamoyl, or (b) -R 1 = H- dehydrogenating the corresponding 5,6-dihydro derivative, any 6H compound being isomerized to the 4H compound, optionally followed in each case by conversion to the 5-oxide or a salt. The 5,6-dihydro derivatives are prepared by converting the corresponding 2-azidobenzophenone to its oxime, reacting the oxime with an acetylenedicarboxylic acid diester, reducing the resulting 1-[2-(α-hydroxyiminobenzyl)phenyl]- 1H - v - triazole - 4,5 - dicarboxylic acid diester to the amine, cyclizing the latter to the corresponding 6 - phenyl - 5,6 - dihydro - 4 - oxo - 4H- v - triazolo[1,5-a][1,4]benzodiazepine - 3 - carboxylic acid ester, hydrolysing the ester, decarboxylatingthe acid and reducing the resulting lactam. The 2-azidobenzophenones are prepared by diazotizing the corresponding 2-aminobenzophenones, followed by reaction with an azide. The 6 - phenyl - 4H - v - triazolo[1,5-a][1,4] benzodiazepines, their 5-oxides and salts are tranquilizers and anticonvulsants, and may be administered in the form of pharmaceutical preparations containing them in association with a carrier. |
| priorityDate | 1972-12-29-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 28.