http://rdf.ncbi.nlm.nih.gov/pubchem/patent/GB-922258-A
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_dc2f7134efa50484bb359fda73782848 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61Q11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K8-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F9-091 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K8-69 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-09 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K8-55 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61Q11-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K8-69 |
filingDate | 1961-06-08-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 1963-03-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | GB-922258-A |
titleOfInvention | Phosphoric acid esters of substituted fluoroalkanols and process for their manufacture |
abstract | The invention comprises compounds of the formula <FORM:0922258/IV(a)/1> where R1 is hydrogen or alkyl of 1-5 carbon atoms, R2 is a free or esterified carboxyl group, a carboxamido group or an ether group, and n is 0 or 1; their salts, and their preparation by reacting a compound <FORM:0922258/IV(a)/2> where R2 is a free or functionally modified carboxyl group or an ether group, with a reactive derivative of phosphoric acid, and if desired, if necessary after conversion of the product into the free phosphoric acid ester, converting into a salt. Suitable reactants are phosphoric acid anhydrides, such as polyphosphoric or pyrophosphoric acids, halides, such as POCl3, and esters, such as diaryl halophosphates. If R1 in the reactant is -CN it is converted by the reaction to -COOH or -CONH2. Examples prepare the calcium salts of (1) a -phosphoroxy-b -fluorolactic acid methyl ester, (2) 3-phosphoroxy-4-fluorobutyramide, (3) 3-phosphoroxy-4-fluorobutyric acid, (4) 2-carboxamido-2-phosphoroxy-3-fluoropropane and (5) 1-guaiacyloxy- 2-phosphoroxy- 3-fluoropropane. The compounds of the invention are useful as pharmaceutical chemicals, especially for caries-inhibiting purposes (see Group VI). 3-Hydroxy-4-fluorobutyronitrile is prepared by reacting 1-chloro-2-hydroxy-3-fluoropropane with KCN in aqueous ethanol. Fluoroacetone cyanohydrin is obtained by addition of HCN to fluoroacetone. 1-Guaiacyloxy- 2-hydroxy- 3-fluoropropane is obtained by reacting guaiacol sodium salt with 1-chloro-2-hydroxy-3-fluoropropane, or by reacting guaiacol with epifluorohydrin. b -Fluorolactic acid methyl ester is obtained by esterifying the acid with diazomethane.ALSO:Pharmaceutical preparations, especially for the care of the teeth, comprise a compound <FORM:0922258/VI/1> where R1 is hydrogen or alkyl of 1-5 carbon atoms, R2 is a free or esterified carboxyl group, a carboxamido group or an ether group and n is 0 or 1 or a salt thereof (see Group IV (b)) in admixture or conjunction with a pharmaceutically suitable carrier, e.g. a toothpaste mixture. Suitable carriers are gelatin, cholesterol, lactose, starch, magnesium stearate, talc, vegetable oils, benzyl alcohol, gums, polyalkylene glycols, and petroleum jelly. The compositions may be made up as tablets, dragees, powders, ointments, creams, solutions, suspensions or emulsions. Preserving, stabilising, wetting or emulsifying agents may also be present. |
priorityDate | 1960-06-08-04:00^^<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: 49.