http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1263035-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3b9f373878f16dc291ff597162e9b344 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C49-255 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D303-22 |
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| filingDate | 1970-07-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1972-02-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1263035-A |
| titleOfInvention | 0,4-methano and 1,4-ethano-tetrahydronaphthyloxypropanols |
| abstract | 1,263,035. 1,4-Methano and 1,4-ethano- 1,2,3,4-tetrahydronaphthyloxypropanols. CARLO ERBA S.p.A. 22 July, 1970 [30 July, 1969; 4 Feb., 1970], No. 35550/70. Heading C2C. Novel compounds of the general Formula I wherein each of the groups R and R<SP>1</SP>, which may be the same or different is a hydrogen or halogen atom or a C 1-4 alkyl, C 1-4 alkoxy, nitro, substituted or unsubstituted amino, C 1-6 alkanesulphonamido, C 1-6 -alkylthio, C 1-6 alkylsulphinyl or C 1-6 alkylsulphonyl group or R<SP>4</SP>R<SP>5</SP>NSO 2 wherein R<SP>4</SP> and R<SP>5</SP> which may be the same or different is a hydrogen or C 1-6 alkyl, or CH 3 (CH 2 ) n CONR<SP>6</SP>- wherein n is 0-6 and R<SP>6</SP> is a hydrogen or methyl; x is 1 or 2; R<SP>2</SP> is hydrogen, C 1-4 -alkyl or a benzyl group; R<SP>3</SP> is hydrogen, C 1-10 alkyl or a benzyl group, and pharmaceutically acceptable salts thereof may be prepared by (a) reacting a compound of the formula II or III where X is a halogen, with an amine HNR 2 R 3 ; (b) reacting a compound of the Formula IV with a compound XCH 2 CHOHCH 2 NR<SP>2</SP>R<SP>3</SP>; (d) catalytically reducing a compound I wherein R<SP>1</SP> is a nitro group to an amino group and optionally acylating to give a Compound I wherein R<SP>1</SP> is alkanesulphonamido or CH 3 (CH 2 ) n CONR<SP>6</SP>-; (e) reacting Compound I wherein R<SP>1</SP> is amino under reductive conditions with formaldehyde to give I wherein R<SP>1</SP> is -NHCH 3 ; (f) reacting a compound of the Formula VI with an amine HNR<SP>2</SP>R<SP>3</SP> and then reducing the reaction product; and optionally (g) reacting Compound I with an appropriate acid to give a pharmaceutically acceptable salt. Compounds II may be prepared by reacting a corresponding hydroxy compound IV with epichlorohydrin to introduce the epoxide side chain, which may in turn be hydrolysed to Compound III. Compounds VI may be prepared by reacting a sodium salt of IV with a 1,3-dihaloacetone. Substituents R 1 may be introduced into Compounds IV by nitration of IV where R 1 is H. Pharmaceutical compositions of Compound I with a carrier or diluent show #-adrenergic receptor blocking activity when administered parenterally. |
| priorityDate | 1969-07-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 51.