http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-779516-A

Outgoing Links

Predicate Object
assignee http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d202e9e866984fe229f6facc38f1d740
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C327-00
filingDate 1955-10-21-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1957-07-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-779516-A
titleOfInvention Alkylsulfonyl-thiobenzoates
abstract The invention comprises ethylthio-p-alkyl-sulphonyl benzoates of the formula <FORM:0779516/IV(b)/1> where R represents an alkyl group containing from one to eight carbon atoms, and a process for their preparation by reacting a p-carboxy-phenyl alkyl sulphone with thionyl chloride and reacting the product with ethyl mercaptan or an alkali metal ethyl mercaptide, preferably in an organic solvent, e.g. chloroform, ether, ethylene dichloride, tetrahydrofuran, benzene, xylene, dimethylacetamide and dimethylformamide. In examples: (1) p-carboxyphenyl ethyl sulphone is refluxed with thionyl chloride and the mixture evaporated to dryness giving p-(ethylsulphonyl) benzoyl chloride, which is then refluxed with ethyl mercaptan in chloroform until no more HCl is evolved, the mixture concentrated and ethylthio-p-(ethylsulphonyl)-benzoate crystallized by the addition of petrol ether. (2) As in (1), replacing ethyl mercaptan by a suspension of sodium ethyl mercaptide. (3) As in (1), replacing ethyl mercaptan sulphone, to yield ethylthio - p - (methylsulphonyl)-benzoate. Starting material. p-Carboxyphenyl ethyl sulphone is prepared by treating toluene p-sulphonyl chloride with aqueous sodium bicarbonate and sodium sulphite, boiling the resultant sodium toluene p-sulphinate with ethyl iodide in aqueous ethanol and oxidizing the p-tolyl ethyl sulphone obtained with potassium permanganate.ALSO:Antitubercular compositions comprise an ethylthio - p - (alkyl sulphonyl) - benzoate, wherein the alkyl group contains from 1-8 carbon atoms, in combination with a pharmaceutical carrier. The compositions may be dispensed as tablets, pills, powders, capsules, granules, suspensions or aerosols, and may contain liquid or solid carriers, e.g. water, oils, starch, sucrose, talc, lactose or alginic acid; also lubricants, binders and disintegrating agents, e.g. mineral oils, magnesium stearate, stearic acid, gum, gelatin, alkali metll bicarbonates and magnesium carbonate. Tablets may further contain artificial flavours, colouring agents, and may be coated, e.g. with sugar or shellac. Aerosols are produced by nebulizing an aqueous solution, oil suspension, or fine particles of the active material, and may be applied from a bomb or pressurized container equipped with a valve for releasing its contents to the atmosphere, containing a gaseous propellant in liquid form, e.g. chlorodifluoroethane, dichlorodifluoromethane, trichlorofluoroethane, trichlorofluoromethane, nitrous oxide or carbon dioxide. The aerosol formulation preferably contains an emulsifying agent, e.g. polysorbate 80, sodium lauryl sulphate, glycol distearate, glycol dioleate, and polyethylene glycols.
priorityDate 1954-11-30-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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