http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-268769-A1
Outgoing Links
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2dbb2d7ecbd600cf89fbdd230f4a466c |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D417-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D225-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D225-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D223-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D413-06 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D403-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D225-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D417-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D223-20 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D225-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D413-06 |
filingDate | 1961-07-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1961-12-16-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | ES-268769-A1 |
titleOfInvention | PROCEDURE FOR THE PREPARATION OF NEW DERIVATIVES OF TETRAHYDRO-5,10,11,12 DIBENZO [B, G] AZOCINE |
abstract | The invention comprises compounds of general formula <FORM:0983859/C2/1> wherein: A represents a straight or branched saturated aliphatic hydrocarbon group containing 1 to 6 carbon atoms Z represents an amino, monoalkylamino, dialkylamino, pyrrolidino, piperidino, morpholino, thiomorpholino, piperazino or N-alkylpiperazino group, or an N-alkylpiperidyl or N-alkylpyrrolidyl group attached to the hydrocarbon radical A by a carbon atom of the heterocyclic nucleus, or a group of general formula <FORM:0983859/C2/2> where R represents a hydrogen atom or a hydroxyalkyl group, n represents 0, 1, 2 or 3 and m represents 2 or 3 B represents hydrogen or a group Z and, where Z or B represents piperazino, N-alkylpiperazino or a piperazino group (IV), then the piperazine ring may be substituted on one or more carbon atoms by an alkyl group, and the word alkyl means an alkyl group containing not more than 4 carbon atoms and their acid addition salts and their preparation by (1) reacting 5,10,11,12-tetrahydrodibenz[b,g]azocine with a compound of formula Y-A(B)-Z where Y represents the acid residue of a reactive ester, (2) reacting a compound of formula HZ with a compound of formula <FORM:0983859/C2/3> where B1 represents hydrogen or a group Y, and (3) decarboxylating a compound of formula <FORM:0983859/C2/4> by heating to a temperature above 100 DEG C. until evolution of carbon dioxide ceases. Other processes referred to are (4) the reaction of compounds of formula <FORM:0983859/C2/5> where T is piperazino and B2 is hydrogen or piperazino, either with a compound of formula YCmH2mOR or with ethylene oxide or propylene oxide, and (5) the reaction of compounds of formula <FORM:0983859/C2/6> where X is <FORM:0983859/C2/7> and B3 is hydrogen or a group X, either with a compound of formula Y-R1, where R1 is hydroxyalkyl, or with ethylene or propylene oxide. Esters (A) above may be prepared from corresponding carboxylic acid halides by reaction with an alcohol of formula HO-A(B)-Z. 5 - (3 - Chloro - 2 - methylpropyl) - 5,10,11,12 - tetrahydrodibenz[b,g]azocine is obtained by reacting the 5-unsubstituted compound with butyl-lithium in ether and adding 1-chloro-2-methyl - 3 - toluene - p - sulphonyloxypropane. 5 - (3 - Chloropropyl) - 5,10,11,12 - tetrahydrodibenz[b,g]azocine is obtained similarly. 5 - (2 - Hydroxyethyl) - 5,10,11,12 - tetrahydrodibenz[b,g]azocin is obtained by reacting the 5-unsubstituted compound with butyl-lithium in ether and adding ethylene oxide. Pharmaceutical compositions comprise compounds (I) and salts of the invention together with pharmaceutical carriers. Oral, parenteral and rectal administration is described (e.g. as tablets, capsules, pills, powders, granules, syrups, elixirs, suspensions, solutions, emulsions, suppositories). The compounds are useful in psychic disorders and as antiemetics, spasmolytics, muscle-relaxants, local anaesthetics, antihistaminics and sedatives. Specification 926,335 is referred to. |
priorityDate | 1960-07-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 48.