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Outgoing Links

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classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-79
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-26
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-79
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D213-26
filingDate 1973-02-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1975-12-17-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1418172-A
titleOfInvention 5-haloalkyl- picolinic acid and process of production thereof
abstract 1418172 5-Haloalkyl-picolinic acids ZAIDAN HOJIN BISEIBUTSU KAGAKU KENKYU KAI 6 Feb 1973 [7 Feb 1972 30 May 1972 1 June 1972 5 Dec 1972] 5861/73 Heading C2C Novel 5-haloalkylpicolinic acids of the general formula wherein R 1 is a C 3-6 alkylene group and X is a halogen atom, provided that the halogen atom is attached to the carbon atom of R 1 furthest from the pyridine ring, are prepared (a) by reacting a 2-methyl-5-haloalkylpyridine of the general formula with a peroxide, reacting the resulting 2-methyl- 5 - haloalkylpyridine - N - oxide with a carboxylic acid anhydride, hydrolysing the resulting 2 - acyloxymethyl - 5 - haloalkylpyridine and oxidizing the resulting 2-hydroxymethyl-5-haloalkylpyridine, optionally via a 5-haloalkylpyridine-2-carboxaldehyde; (b) by reacting a 2- methyl-5-haloalkylpyridine of the second general formula above with benzaldehyde in the presence of a dehydrating agent and oxidizing the resulting 2-styryl-5-haloalkylpyridine; and (c) by oxidizing a 2-methyl-5-haloalkylpyridine of the second general formula above with selenium dioxide. 2 - Methyl - 5 - haloalkylpyridines of the second general formula above (optionally isolated as picrates) are prepared (a) by reacting a 2 - methyl - 5 - hydroxyalkyl - pyridine with ptoluenesulphonyl halide in anhydrous pyridine for a long period of time or with a thionyl halide in pyridine; (b) when X is a chlorine atom, by reacting 2-methyl-5-ethynylpyridine with sodamide, followed by a compound of the general formula Cl-R 1 -Br, followed by catalytic reduction; (c) when X is a chlorine atom, by reacting 2-methyl-5-ethynylpyridine with sodium, followed by a chloroalkyl p-toluenesulphonate; and (d) when X is a fluorine atom, by reacting the corresponding 2-methyl-5- chloroalkylpyridine with potassium fluoride. Pharmaceutical compositions having hypotensive activity comprise, as active ingredient, a 5- haloalkylpicolinic acid of the first general formula above, together with a pharmaceutically acceptable carrier or diluent.
priorityDate 1972-02-07-04:00^^<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: 33.