http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-366784-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_14effe3850d2129f863b969dac4f1db8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D281-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D267-20 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D281-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D267-20 |
| filingDate | 1969-05-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1971-12-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-366784-A1 |
| titleOfInvention | PROCEDURE FOR PREPARING 11-AMINODIBENZ (B, F) (1,4) OXA (TIA) ZEPINAS. |
| abstract | Novel dibenzoxazepines and dibenzothiazepines of Formula I in which X is oxygen or sulphur, R 1 is hydrogen, C 1-4 alkyl or hydroxy-C 1-4 alkyl and R 2 is cyano, di-(C 1-4 alkyl)-sulphamoyl, C 2-5 alkanoyl, [alpha]- chlorovinyl or C 1-4 alkoxy-carbonyl, and non- toxic acid addition salts thereof, are prepared by (a) cyclizing a compound of Formula II in which X1 is oxygen or sulphur, Z is the group of Formula III or OH, halogen, OSO 2 Ar, SH, SR, amino or substituted amino, Ar being aryl and R being alkyl, and, when required, before or after cyclization, converting Z from OH, halogen, OSO 2 Ar, SH, amino or substituted amino, to a group of Formula III, or (b) reacting a compound of Formula IV in which Q is halogen, OH, OSO 2 Ar, SH, SR, amino or substituted amino, with a compound of Formula V or (c) cyclizing a compound of Formula VI in which X1 is O or S, or (d) cyclizing a compound of Formula VI A in which one of W and Z is OH or SH and the other is H, NO 2 , halogen or diazonium, or (e) using the following reaction scheme in which R 4 is CN, sulphinic acid (-SO 2 H) or [alpha]-oximino-C 1-4 alkyl Compounds IA are prepared by treating the diazonium salt with KCN and an appropriate catalyst, with sulphur dioxide and copper powder or a ferrous salt, or with an alkanal oxime. The sulphinic compounds IA can be converted to compounds I, R 2 = dialkylsulphamoyl, by oxidation, halogenation and reaction with a dialkylamine. The oximinoalkyl compounds IA can be converted to compounds I, R 2 = C 2-5 alkanoyl, by hydrolysis. The preparation of the following intermediates is described: p - (o - nitrophenoxy) - acetophenone, p - (o - aminophenoxy)acetophenone, p - acetoxybenzenesulphonyl chloride, N,N- dimethyl - p - hydroxybenzenesulphonamide, N,N - dimethyl - p - (o - nitrophenoxy)benzenesulphonamide, o - (p - dimethylsulphamoylphenozy)aniline, o - (p - dimethylsulphamoylphenoxy)carbanilate, 21 - (p - dimethylsulphamoylphenoxy) - 4 - methyl - 1 - piperazinecarboxanilide hydrochloride, ethyl o - (p - acetylphenoxy) - carbanilate, 21 - (p - acetylphenoxy)- 4 - methyl - 1 - piperazine carboxanilide and its hydrochloride, 4 - (N,N - dimethylsulphamoyl)- diphenyldisulphide, 4 - mercapto - N,N - dimethylbenzenesulphonamide, o.(p-dimethylsalphamoyl phenyl)aniline, p - (o - aminophenylthio)acetophenone, ethyl o - (p - dimethylsulphamoylphenylthio)carbanilate, 21- (p - dimethylsulphamoylphenoxy) - 1 - piperazine carboxanilide, 11 - (4- methyl - 1 - piperazinyl) - 2 - ([alpha] - oximinopropyl)- dibenz[b,f][1,4]oxazepine, -ethyl o - (o - nitrophenoxy)benzoate and ethyl p - (o - amino - phenoxy)benzoate. Pharmaceutical compositions for oral or parenteral administration, comprise a compound of Formula I or an acid addition salt thereof together with a carrier. Compounds I and their salts have central nervous system and analgesic properties. |
| priorityDate | 1967-02-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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