http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-1106742-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6b6fc801b5bfe5304ffa40d938db6e09 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-72 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D227-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D491-10 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D227-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-72 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D491-10 |
| filingDate | 1965-03-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 1968-03-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | GB-1106742-A |
| titleOfInvention | New piperidine derivatives and the homologues thereof and process for their production |
| abstract | Compounds of the formula <FORM:1106742/C2/1> wherein X represents an oxo group or the groups <FORM:1106742/C2/2> wherein R1 is an alkyl radical containing at most 7 carbon atoms and R2 is a divalent hydrocarbon radical containing 2 to 10 carbon atoms; Y represents the oxo group or the group <FORM:1106742/C2/3> wherein R4 is an alkylene radical which is preferably saturated and contains at most 5 carbon atoms; R represents hydrogen or a methyl radical; and n represents 0, 1 or 2 and their salts with inorganic and organic acids and preparation thereof by condensing a compound of the formula <FORM:1106742/C2/4> wherein X, R and n have the above significance with a suitable reactive ester derived from a compound of the formula <FORM:1106742/C2/5> wherein Y has the above meaning, in an organic solvent in the presence of an acid binding agent with optional subsequent hydrolysis to an oxo group of one or both of the groups X and Y when these symbols represent ketal groups and, if desired, with further selective re-introduction of different ketal groups. Substituted 4-piperidone derivatives of the second general formula above, wherein X represents <FORM:1106742/C2/6> and R2 has the aforementioned significance, are prepared by condensing 4,4-dihydroxypiperidine hydrochloride with a suitable dihydric alcohol in the presence of p-toluenesulphonic acid. Pharmaceutical compositions suitable for oral, rectal or parenteral administration, comprising as active ingredient at least one compound of the first general formula above or a pharmaceutically acceptable organic or inorganic acid addition salt in association with at least one pharmaceutical carrier, act as calmatives, psychoregulators or sedatives. The preparation of 1-[41-(p-fluorophenyl)-41-oxo - 11 - butyl] - 4,4 - ethylenedioxy-piperidine, [4 - (p-fluorophenyl) - 41,41 - ethylenedioxy - 11-butyl] - 4,4 - ethylenedioxy - piperidine, 1 - [41-(p-fluorophenyl) - 41 - oxobutyl] - 4,4 - ethylenedioxy-piperidine, 1 - [(41 - p - fluorophenyl) - 41 - oxo - 11 - butyl] - 4 - piperidone, 1 - [41 -p-fluorophenyl - 41 - oxobutyl] - 4,4 - dihydroxy-piperidine and 1 - [(41 - p - fluorophenyl) - 41-oxo -11 - butyl] - 4,4 - diethoxy - piperidine is given and numerous other compounds corresponding to the first general formula above are described. 1 - (p-Fluorophenyl) - 1,1 - ethylenedioxy - 4-chlorobutane and 2 - (p - fluorophenyl) - 2 - (3-chlorobutyl) - 4 - methyl - m - dioxan are obtained by ketalization of p-fluoro-g -chlorobutyrophenone with the appropriate dihydric alcohol in the presence of p-toluenesulphonic acid. 4,4-Dimethoxypiperidine is prepared by reacting 4,4-dihydroxypiperidine hydrochloride with methyl alcohol in the presence of p-toluenesulphonic acid. p-Fluoro-g -chlorobutyrophenone is prepared by a Friedel-Crafts reaction between fluorobenzene and g -chlorobutyric acid. |
| priorityDate | 1964-03-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 42.