http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2015119259-A
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-28 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-75 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D239-28 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07F5-025 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-14 |
| filingDate | 2013-10-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2016-12-20-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2015119259-A |
| titleOfInvention | IMPROVED METHOD FOR PRODUCING 5- (2,6-DI-4-MORPHOLINYL-4-PYRIMIDINYL) -4-TRIFTORMETHYLPYRIDIN-2-AMINE |
| abstract | 1. A method for producing a compound of formula A, comprising the steps of: (a) acylating 5-bromo-4- (trifluoromethyl) pyridin-2-amine to form N- (5-bromo-4- (trifluoromethyl) pyridin-2-yl) acetamide; ( b) the interaction of N- (5-bromo-4- (trifluoromethyl) pyridin-2-yl) acetamide with a Grignard alkyl reagent, followed by the addition of trialkyl borate and 2,2'-azanediyl diethanol in an organic solvent to form N- (5- (1, 3,6,2-dioxazaborocan-2-yl) -4- (trifluoromethyl) pyridin-2-yl) acetamide; (c) a combination of N- (5- (1,3,6,2-dioxazaborocan-2-yl) -4- (trifluoromethyl) pyridin-2-yl) acetamide with 4.4 '- (6-chloropyrimidin-2,4-d iyl) di [morpholine] via the palladium-catalyzed Suzuki coupling reaction to form N- (5- (2,6-dimorpholinopyrimidin-4-yl) -4- (trifluoromethyl) pyridin-2-yl) acetamide; and (d) hydrolyzing N- (5- (2,6-dimorpholinopyrimidin-4-yl) -4- (trifluoromethyl) pyridin-2-yl) acetamide under an acidic medium to form a compound of formula A.2. The method of claim 1, wherein the Grignard alkyl reagent of step (b) is lithium isopropyl magnesium chloride in tetrahydrofuran and the trialkyl borate is triisopropyl borate. 3. The method of claim 2, wherein the palladium-catalyzed Suzuki combination of step (c) comprises generating a palladium catalyst in situ from palladium acetate and triphenylphosphine in an organic solvent. The method of claim 3, wherein the hydrolyzed N- (5- (2,6-dimorpholinopyrimidin-4-yl) -4- (trifluoromethyl) pyridin-2-yl) acetamide is treated with N-acetyl-L-cysteine. A compound that is N- (5- (1,3,6,2-dioxazaborocan-2-yl) -4- (trifluoromethyl) pyridin-2-yl) acetamide. 6. A compound that is N- (5- (1,3,6,2-dioxazaborocan-2-yl) -4- (trifluoromethyl) pyridin-2-yl) amine. 7. A process for preparing a compound of formula A, comprising the steps of: (a) reacting 5-bromo-4- (trifluoromethyl) pyridin-2-amine with an alkyl reagent |
| priorityDate | 2012-10-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 66.