http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-898045-A

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assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_3a5173a7d063a9f70ca7b5e86fc23863
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-088
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-092
filingDate 1959-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b485740c51cd4ed0c6749e4e07419fd3
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e02c10590798b9c6323da5ffea9766a9
publicationDate 1962-06-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-898045-A
titleOfInvention Nuclearly substituted anilines and nitrobenzenes and their preparation
abstract The invention comprises substituted benzenes of the formula <FORM:0898045/IV (b)/1> (wherein R is a hydrocarbon radical of at most 8 carbon atoms, Z is NO2 or NHY, Y being hydrogen or alkanoyl of at most 6 carbon atoms, X is an alkylene radical of 2, 3 or 4 carbon atoms and has its valencies on different carbon atoms and NB is dialkylamino wherein each alkyl group contains at most 6 carbon atoms or piperidino or 1-pyrrolidinyl which may be substituted by alkyl radicals containing at most 4 carbon atoms) and their acid-addition salts; and their preparation by reacting an appropriate halo-(RO)-nitro-phenol with an appropriate tertiary aminoalkyl halide and when required reducing the nitro compound to an amino compound and, when required, acylating this. Alternatively an appropriate halo-alkyl halide can be used as the second reaction component and the product reacted with a tertiary amine. Examples are given and a list of saltforming organic and inorganic acids is provided. Compounds of the formula <FORM:0898045/IV (b)/2> wherein the halogen is chlorine, bromine or iodine are prepared (1) by halogenating an appropriate (RO)-nitro-phenol; or (2) by nitrating an appropriate (RO)-halo-phenol; or (3) by reacting an (RO)-halo-hydroxy-benzaldehyde with fuming nitric acid. When the halogen is fluorine they are prepared by diazotizing an (RO)-amino-nitro-phenol, reacting the diazonium salt with fluoboric acid to form the diazonium fluoborate and heating this. 2-n-Propoxy-4-nitrophenol is prepared by reacting catechol with n-propyl benzene sulphonate to form 1,2-di-n-propoxy-benzene, nitrating this to 1,2-di-n-propoxy-4-nitrobenzene and monodealkylating this. The corresponding methoxy, ethoxy, butoxy, hexoxy and benzyloxy compounds are prepared similarly.ALSO:Substituted benzenes of the formula <FORM:0898045/VI/1> (wherein R is a hydrocarbon radical of at most 8 carbon atoms, Z is NO2 or NHY, Y being hydrogen or alkanoyl of at most 6 carbon atoms, X is an alkylene radical of 2, 3 or 4 carbon atoms and has its valencies on different carbon atoms and NB is dialkylamino wherein each alkyl group contains at most 6 carbon atoms or piperidino or 1-pyrrolidinyl which may be substituted by alkyl radicals containing at most 4 carbon atoms) or salts thereof with organic or inorganic acids, may be formulated as local anaesthetic compositions. Conveniently, the salts are used in aqueous preparations for topical administration or intramuscular or intravenous injection. The active compounds may advantageously be combined with other pharmacologically active compounds, e.g. vasoconstrictor agents.
isCitedBy http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0926119-A1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6399837-B1
http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6124507-A
priorityDate 1959-05-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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