http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102030716-A
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_d94573ab2c57e8b193f3a22accddf9fe |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D239-94 |
| filingDate | 2009-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_48bd3ac147f8557aa28ae7521b7e270b http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d5bcf7e1988203e23c2885c7d1c86e38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_00c38c928fe6e4fb837f97bdb88b57fa |
| publicationDate | 2011-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-102030716-A |
| titleOfInvention | Method for preparing gefitinib |
| abstract | The invention discloses a novel preparation method for synthesizing gefitinib. 3,4-dimethoxybenzoic acid (2) is taken as a raw material, and the method comprises the following steps of: nitrifying, demethylating and methylating the 3,4-dimethoxybenzoic acid (2) to prepare an intermediate of 2-nitryl-4-methoxy-5-methyl-hydroxybenzoate (5); reacting the intermediate with 4-(3-bromopropyl) morpholine, and introducing an alkyl side chain to prepare an intermediate 6; reducing nitryl, and performing ring formation with methanamide to construct a quinoline matrix ring 8; halogenating 4-carbonyl by using the compound 8 under the action of thionyl chloride to generate an intermediate 9; and reacting with halogen substituted aromatic amine 3-chloro4-fluoroaniline to obtain the target product of gefitinib (1). In the method, the selected initial raw material is low in cost, the synthesizing route is simplified, and the raw material utilization rate and the total yield are greatly improved. The intermediates obtained in the reactions are mostly purified by a re-crystallization method, or directly subjected to the next reaction, so the yield is high, a few three wastes are generated in the reaction process, the cost is low and the method is favorable for industrial production. |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102584720-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102584720-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103910689-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103910689-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103864719-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103524433-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110747489-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-110747489-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103755648-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103755648-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103319422-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103319422-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-105218476-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-108727284-B http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-108727284-A |
| priorityDate | 2009-09-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 43.