http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-109748902-B
Outgoing Links
Predicate | Object |
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classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 |
filingDate | 2017-11-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 2020-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationDate | 2020-11-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CN-109748902-B |
titleOfInvention | Preparation method of erlotinib hydrochloride |
abstract | The invention discloses a preparation method of aritinib hydrochloride, which comprises the steps of directly butting 7-benzyloxy-4-chloro-6-methoxyquinoline compound 1 and 1- (2-fluoro-3-hydroxy-6-nitrophenyl) propyl-2-ketone compound 2 serving as initial raw materials to obtain a compound 3, and developing a compound 3The two methods synthesize the compound 5 through a single-step or two-step reaction, and the reduction of the nitro group and the removal of the benzyl protecting group are completed in one step in the hydrogenation reaction, thereby greatly simplifying the reaction route. Meanwhile, the protecting group of the cyclopropylamine fragment 6 is optimized and the Boc protecting group is selected, so that the subsequent deprotection reaction avoids palladium catalytic hydrogenation, the heavy metal residue of the final product is favorably reduced, the salt formation process can be completed in a one-pot method, the route efficiency is greatly improved, the process cost is reduced, the generation of byproducts is reduced, the purity of the final finished product is favorably improved, and the synthetic route is synthesized: |
priorityDate | 2017-11-02-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 141.