http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0158545-B1
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-265 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-265 |
| filingDate | 1985-03-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 1987-04-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1987-04-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-0158545-B1 |
| titleOfInvention | [Alpha-(alkylaminomethyl)-benzylthio]-acetic-acid derivatives, process for their preparation and their therapeutic use |
| abstract | For the contracting States BE, CH, DE, FR, GB, IT, LI, LU, NL, SE 1. A amine derivative of (benzylthio)acetic acid, characterized in that it is selected from the group consisting of a) [alpha-(alkylaminomethyl)-benzylthio]-acetic acid derivatives of the general formula : see diagramm : EP0158545,P13,F1 wherein X is S or SO, Y is C1 -C4 -alkoxy, NH2 or NHOH, Z is C1 -C4 -alkyl, R is H or CH3 , R1 and R2 , which may be the same or different, represent each H, F, Cl, Br ; b) their optical isomers, and c) addition salts thereof. For the contracting State : AT 1. A method for preparing a [alpha-(alkylaminomethyl)-benzylthio]-acetic acid derivative of the formula : see diagramm : EP0158545,P14,F1 wherein X is S or SO, Y is C1 -C4 -alkoxy, NH2 or NHOH, Z is C1 -C4 -alkyl, R is H or CH3 , R1 and R2 , which may be the same or different, represent each H, F, Cl, Br ; its optical isomers and addition salts thereof, said method being characterized in that it comprises the following steps : a) reacting a N-alkyl-N-(2)halogeno-2-phenylethyl)-amine of the formula : see diagramm : EP0158545,P14,F2 wherein Hal represents F, Cl or Br, Ar represents a (R1 R2 )C6 H3 group in which R1 and R2 are defined as indicated above, and Z is defined as indicated above, with an alkyl thioglycolate of the formula HS-CHR-CO-A wherein A is C1 -C4 -alkoxy and R is H or CH3 , in an alcohol of the formula : H-A wherein A is defined as indicated above, in the presence of an alcaline metal, at a temperature comprised between room temperature and the reflux temperature of the reaction medium, for obtaining an alkyl [alpha-(alkylaminomethyl)-benzylthio]-acetate of the formula : see diagramm : EP0158545,P14,F3 b) if needed, reacting, for at least 5 h a temperature of between 15 and 25 degrees C, said alkyl [alpha-(alkylaminomethyl)-benzylthio]-acetate thus obtained with a compound selected from NH3 and NH2 OH for obtaining, respectively, the corresponding amide of the formula : see diagramm : EP0158545,P14,F4 and hydroxamic acid of the formula : see diagramm : EP0158545,P14,F5 and c) if needed, subjecting the sulfide compound selected from the group consisting of compounds of the formulae V, VI and VII, to an oxidation reaction with H2 O2 in order to obtain a sulfinyl compound of the formula I in which X is SO. |
| priorityDate | 1984-03-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 57.