http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-931789-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_035d1cf7a2fed40b7fbac68b3cced081 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-36 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-64 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-64 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-36 |
| filingDate | 1961-03-13-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1963-07-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-931789-A |
| titleOfInvention | Improvements in or relating to 4-arylpiperidine derivatives |
| abstract | The invention comprises compounds of the formula <FORM:0931789/IV(a)/1> wherein Alk is an alkylene radical of 3 to 6 carbon atoms, Ar is phenyl which may be substituted by one halogen atom or alkyl or methoxy group or by two methyl groups, or is thienyl, Ar1 is a phenyl or substituted phenyl radical or thienyl radical similar to Ar but may also be substituted by a tri-fluoromethyl group, R is amino, mono- or di-alkyl-amino, anilino, N-methyl-anilino, benzylamino, pyrrolidino, piperidino, morpholino, mono- or di-methylmorpholino, piperazino or phenyl-piperazino, and X is a hydrogen atom or a methyl group. They may be prepared by condensation of an appropriate aroylalkyl halide with an appropriate 4-arylpiperidine carboxamide. Examples are given and salts with inorganic and organic acids and quaternary ammonium derivatives with alkyl, aralkyl, hydroxyalkyl and alkenyl halides, sulphates and aryl sulphonates are described. Aroylalkyl halides Ar-CO-Alk-Hal are prepared by Friedel Crafts reaction between a halo-alkyl halide and a benzene or a substituted benzene or thiophene; or by treating an o -haloalkanonitrile with the appropriate arylmagnesium bromide and then hydrolysing. Substituted piperidines of the formula <FORM:0931789/IV(a)/2> are prepared by condensing HO-(CH2)2-NH-CH2-CH(X)-OH with Y-Cl (Y being a blocking group such as p-toluenesulphonyl or benzyl) to give compounds of the formula <FORM:0931789/IV(a)/3> heating these with thioyl chloride to give the corresponding dichloro compounds, possibly as their hydrochlorides, reacting these with nitriles of the formula Ar1-CH2-CN in presence of sodamide to give nitriles of the formula <FORM:0931789/IV(a)/4> possibly as their hydrochlorides, and simultaneously hydrolysing and detosylating these to give compounds of the formula <FORM:0931789/IV(a)/5> possibly as their hydrochlorides, or hydrolysing them to give compounds of the formula <FORM:0931789/IV(a)/6> possibly as their hydrochlorides, converting these to the corresponding acid chlorides, reacting these with the amines HR to give compounds of the formulae <FORM:0931789/IV(a)/7> <FORM:0931789/IV(a)/8> possibly as their hydrochlorides, and detosylating or debenzylating these. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AU-686760-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5756520-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8084623-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/WO-9521821-A1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-4904673-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5364867-A |
| priorityDate | 1960-03-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 49.