http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102485726-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_e0b5193c00731d77fb5ce1ed7ba178e6 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F7-18 |
| filingDate | 2010-12-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2015-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d64a0c2f27bff4e5d408cfe85c74a243 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9d5ba28f122459f116863122243f9acd http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7af3365017366c9adae474a71ec090a4 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_659987f438f4337a9313071e00c621ef http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_73e9b09d131529a08bde537af36c7d92 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1828be5b8cdf3e1c43e93019edd00b0a |
| publicationDate | 2015-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-102485726-B |
| titleOfInvention | Method for preparing 1-R-1'-spiro-(piperidine-4,4'-quinoline)-2'(3'-hydrogen) ketone |
| abstract | The invention relates to a method for preparing 1-R-1'-spiro-(piperidine-4,4'-quinoline)-2'(3'-hydrogen)ketone, for solving the technical problem that present synthetic methods are not abundant enough. The preparation method comprises the following steps: using 1-tert-butyl oxycarbonyl-4-piperidone as a raw material, adding a condensation catalyst and ethyl cyanoacetate in a solvent to generate reflux reaction, and purifying to obtain a compound 1, that is, 4-((ethoxycarbonyl cyan)methylene)piperidine-1-carboxylic acid tert-butyl ester; reacting the compound 1 with an isopropyl grignard reagent and o-Fluoro bromobenzene under the catalysis of metal halides to obtain a compound 2, that is, 4-((ethoxycarbonyl cyan)methyl)-4'-((2-fluoro)phenyl)piperidine-1-carboxylic acid tert-butyl ester, hydrolyzing the compound 2 under a condition of alkaline reagents to obtain a compound 3, that is, 4-(carboxyl cyan) methyl)-4'-((2-fluoro)phenyl)piperidine-1-carboxylic acid tert-butyl ester; reacting the compound 3 with cuprous oxide or copper powder and carrying out decarboxylation to obtain a compound 4, that is, 4-(ethyl cyan)-4'-((2-fluoro)phenyl)piperidine-1-carboxylic acid tert-butyl ester; hydrolyzing the compound 4 under a condition of hydrogen peroxide/alkaline reagents to obtain a compound 5, that is, 4-(acetamido)-4'-((2-fluoro)phenyl)piperidine-1-carboxylic acid tert-butyl ester; cyclizing the compound 5 with an alkaline reagents/DMF system to obtain a target product. |
| priorityDate | 2010-12-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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