http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-102898449-B
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_8c7c582c58ebb902c3111171ec32c641 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F5-02 |
| filingDate | 2012-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2015-06-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_15eac2b2e4aad5e83523f35756f58603 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_a7d751088e178b972afc0e88abe3a8d7 |
| publicationDate | 2015-06-03-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-102898449-B |
| titleOfInvention | Method for synthesizing Crizotinib intermediate |
| abstract | The invention belongs to the technical field of medicine synthesis, and in particular relates to a method for synthesizing a Crizotinib intermediate. The method comprises steps of: a) reacting a raw material 4-mesylate piperidine-1-formic acid tert-butyl ester (2) with 4-nitro pyrazole to prepare a compound 3; b) reducing nitro by using hydrazine hydrate to obtain an amino compound 4; and c) diazotizing the compound 4 by using tert-butyl nitrite, and reacting the compound 4 with a boric acid ester compound 5 in the presence of a free radical initiator benzoyl peroxide, so as to prepare the Crizotinib intermediate (1). Compared with an existing synthesis method, the method provided by the invention has the following advantages: a diazotization method is used to synthesize the boric acid ester product; and compared with an existing Miyaura boronation method catalyzed by Pd, the method avoids the usage of expensive palladium catalyst and ligand, and has the merits of mild reaction condition, high yield, simple operation, cheap and easily available raw materials and short reaction period, and is quite easy for industrialized mass production. |
| priorityDate | 2012-09-21-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 121.