http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2010123003-A
Outgoing Links
Predicate | Object |
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classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P31-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 |
filingDate | 2008-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2011-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | RU-2010123003-A |
titleOfInvention | METHODS FOR PRODUCING AND INTERMEDIATE COMPOUNDS FOR PRODUCING AMINOBENZYMIDAZOLMETA |
abstract | 1. The method of obtaining 1-ethyl-3- (5- (5-fluoropyridin-3-yl) -7- (pyrimidin-2-yl) -1H-benzo [d] imidazol-2-yl) urea of the formula 1:! ! including! i) the provision of 3-fluoro-5- (4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl) pyridine (formula 2) and 4-bromo-2-nitro-6- (pyrimidine -2-yl) benzeneamine (formula 3),! ! ii) the cross-combination of the compounds of formula 2 and the compounds of formula 3 in a two-phase mixture containing water, an organic solvent, a base and a transition metal catalyst to obtain 4- (5-fluoropyridin-3-yl) -2-nitro-6- (pyrimidine- 2-yl) benzeneamine of the formula 4,! ! iii) reduction of a compound of formula 4 to obtain 5- (5-fluoropyridin-3-yl) -3- (pyrimidin-2-yl) benzene-1,2-diamine of formula 5,! ! iv) reacting a compound of formula 5 with a compound of formula 6,! ! in a two-phase mixture containing buffer water and an organic solvent to obtain a compound of formula 1.! 2. The method according to claim 1, in which the organic solvent in item ii) is an aprotic solvent. ! 3. The method according to claim 2, wherein said aprotic solvent is 1,2-dimethoxyethane or dioxane. ! 4. The method according to claim 1, in which the base according to ii) is an inorganic base. ! 5. The method according to claim 4, in which the specified inorganic base is selected from potassium carbonate, cesium carbonate and potassium phosphate. ! 6. The method according to claim 1, in which the transition metal catalyst according to item ii) is a palladium based catalyst. ! 7. The method according to claim 6, in which the palladium-based catalyst is palladium (II) acetate, tetrakis (triphenylphosphine) palladium (0) or tris (dibenzylideneacetone) dipalladium (0). ! 8. The method according to claim 1, wherein the biphasic mixture indicated in paragraph ii) further comprises a phosphine ligand. ! 9. The method according to claim 8, in k� |
priorityDate | 2007-11-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 75.