http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-986873-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| filingDate | 1963-05-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1965-03-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-986873-A |
| titleOfInvention | 1,4-benzodiazepine derivatives and a process for the manufacture thereof |
| abstract | The invention comprises compounds of the general formula <FORM:0986873/C2/1> wherein R stands for a lower alkyl thio group and wherein the broken line denotes that the 1-(lower alkyl) group is optional, and acid addition salts thereof, and the preparation thereof either by reaction an amino-benzophenone of the formula <FORM:0986873/C2/2> wherein R has the significance given earlier, with glycine or an ester thereof, preferably by heating in a solvent such as pyridine or N,N-dimethylformamide in the presence of an ion of a strong acid (it is convenient to use the starting materials or solvents in the form of their acid addition salts with a strong organic or inorganic acid, e.g. the hydrochloride), or by reacting the said amino - benzophenone with halo - acetyl halide of the formula <FORM:0986873/C2/3> and treating the resultant haloacetamido-benzophenone with ammonia, optionally heating to speed cyclization, and in either case converting the resulting 1,4-benzodiazepine into an acid addition salt if desired. The term "lower" used above means groups containing from 1-7 carbon atoms and the term halogen includes chlorine, bromine, iodine and fluorine. The amino-benzophenones of the second general formula above may be prepared by reacting an appropriately substituted 2-amino-(21,31- or 41-halo)-benzophenone with a sodium lower alkyl mercaptan. In an example o-fluoro-benzoyl chloride and p-chloro-aniline are heated in the presence of zinc chloride to give 2-amino-5-chloro-21-fluoro-benzophenone which is then reacted with sodium methylmercaptan in 2-ethoxy-ethanol under reflux to yield 2-amino-5-chloro-21-methylthio-benzophenone. Pharmaceutical preparations having sedative, tranquillizing, muscle relaxing and anticonvulsant effects for enteral or parenteral administration comprising a compound of the first general formula above and one or more inert solid or liquid carriers or diluents. |
| priorityDate | 1962-05-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 44.