http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102617487-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_4c0ed78c4d5c4951a22374d61ea1f178 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P31-18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-557 |
| filingDate | 2012-03-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2014-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2e07fc44c241ff239ff97ee4cdee7f5b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_553ce16fcf2b675056f17842d483f4d6 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_86aa80b5f185f6b034bf66890afdf05e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3029186b7427e55ba4043c164f3048a3 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_dc66263cf443aa37084ef1b94df9e29c http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e7de816b6a41fd25557bca8820b755be |
| publicationDate | 2014-04-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-102617487-B |
| titleOfInvention | Multi-substituted pyrimidinones compounds as well as preparation method and application thereof |
| abstract | The invention relates to multi-substituted benzamides compounds as well as a preparation method and the application thereof, wherein, the multi-substituted benzamides compounds are expressed as N-((4-(1-methyl-2-substituted benzyl-5-methoxy-6-oxo-1,6-dihydropyrimidine-4-carbonyl) piperazidine-1-yl) alkyl) shown in the formula (I). In the formula (I), R1 represents -H or -Cl, R2 represents -H or -Cl or -F or -CH3 or -OH, R3 and R4 represent-OH, R5 represents -H or -OH, and n equals to 2 or 3. The method comprises the steps as follows: oxammonium hydrochloride and substituted phenylacetonitrile can synthesize N'-hydroxyl-2-substituted phenyl acetamidine compounds at first; then the N'-hydroxyl-2-substituted phenyl acetamidine compounds react with dimethyl acetylenedicarboxylate to synthesize 2-(1-amino substituted phenyl ethylidene amino) oxo butadiene diacid dimethyl compounds; 2-(1-amino substituted phenyl ethylidene amino) oxo butadiene diacid dimethyl compounds are processed through cyclization and methylation and then are processed through hydrolyzation and acidification so as to generate formate compounds; then formate compounds react with N-piperazinyl alkyl substituted benzamide to generate N-((4-(1-methyl-2-substituted benzyl-5-methoxy-6-oxo-1,6-dihydropyrimidine-4-carbonyl)piperazidine-1-yl)alkyl)-3,4-dimethoxy-5-substituted benzamide; and finally, demethylation is performed to generate the compounds shown in the formula (I). The multi-substituted benzamides compounds achieve a restraining effect on HIV-1 (Human immunodeficiency virus-1) integrase. |
| priorityDate | 2012-03-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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