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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-584
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D213-89
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-06
http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00
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classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-635
http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-06
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filingDate 2018-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2022-08-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 2022-08-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber CN-109053565-B
titleOfInvention N-benzenesulfonyl-substituted asymmetric pyridine-piperidone compound and preparation method thereof
abstract N-benzenesulfonyl-substituted asymmetric pyridine-piperidone compounds and preparation methods thereof, the present invention relates to nine N-substituted benzenesulfonyl-substituted 3,5-diarylmethylene groups with antitumor and anti-inflammatory activities The ‑4‑piperidone compound belongs to the technical field of anti-tumor and anti-inflammatory drugs. The preparation method of the method is as follows: firstly, 4-piperidone hydrochloride is subjected to Claisen-Schmidt condensation reaction with 2-fluorobenzaldehyde and 4-pyridine aldehyde respectively, and column chromatography obtains the intermediate 4-pyridine-substituted 3, 5-diarylmethylene-N-H-4-piperidone hydrochloride (BAP-H), then, with R The benzenesulfonyl chloride substituted benzenesulfonyl chloride generates benzenesulfonylation to obtain asymmetric N-substituted benzenesulfonic acid Acyl-3,5-diarylmethylene-4-piperidone compound (BAP 1-9). The compound has good anti-tumor and anti-inflammatory activities, can avoid the genotoxicity of currently used anti-tumor drugs, has low toxicity to normal cells, and has anti-inflammatory activity at the same time. The preparation method has the advantages of simple operation, mild reaction conditions and high synthesis yield, which are favorable for its wide popularization in the fields of anti-tumor and anti-inflammatory.
priorityDate 2018-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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