http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2478637-C2
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_b545bd1d6e99ca9634d28326446893ff |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-28 |
| filingDate | 2011-03-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2013-04-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_34b43cb6fbe01ee33a084bcec237dc74 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b6010d1a71ff83ebd0023d862b9a4212 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c1e4df96f6a3fb6c1c3df2eb0901cb59 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d789b1df9f887e1cba77d98fe53413ac http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b295a2e1cf5b2fb7f451c6ddc8767d35 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_40d85e33874e6eb285bdf0c05f6ac753 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_95a58a8348f32bcdca800dae6896da52 |
| publicationDate | 2013-04-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | RU-2478637-C2 |
| titleOfInvention | METHOD FOR PREPARING 5,8,9,10-TETRAHYDROPYRIMIDINO[4,5-d]AZOCINE DERIVATIVES HAVING TRIFLATE, SECONDARY AND TERTIARY AMINO GROUPS IN 4-TH POSITION |
| abstract | FIELD: medicine, pharmaceutics. n SUBSTANCE: invention refers to producing new 5,8,9,10-tetrahydropyrimido[4,5-d]azocine derivatives having triflate, secondary and tertiary amino groups in the 4th position of general formula specified below. In general structural formula: 2-12 2 X=OTf (Tf means triflate), X means NR 1 R2 2 related to the groups 3-12 n n n n n n n n . n The method consists in the fact that 6-isopropyl-2-phenyl-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4(3H)-one reacts with methyl propyolate in methanol at room temperature to produce methyl 8-isopropyl-4-oxo-2-phenyl-5,8,9,10-tetrahydropyrimido[4,5-d]azocine-6-carboxylate (1). Thereafter, the prepared compound reacts with triftalane hydride in dichloromethane in the presence of pyridine at t°=-10°C; it is recovered and purified with by means of column chromatography to prepare methyl 8-isopropyl-2-phenyl-4-{[(trifluoromethyl)sulphonyl]oxy}-5,8,9,10-tetrahydropyrimido[4,5-d]azocine-6-carboxylate (2); then the solution I mmole of the prepared product (2) in absolute dioxide is added with 2 mmole of K 2 CO 3 and 1.5 mmole of appropriate amine. After being boiled for two hours and removing the solvent, respective 4-amino substituted 5,8,9,10-tetrahydropyrimido[4,5-d]azocine of formula 3-12 is prepared. The method is directed to prepare the products in the form of white or yellow powder, or in the form of drying oil. n EFFECT: after the primary screening, the compounds appeared to be acetyl- and butyrylcholin esterase inhibitors and can find application as scaffolds in searching the preparations for treating neurodegenerative diseases. n 10 ex |
| priorityDate | 2011-03-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 120.