http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2352958-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_46830b651781109964ac264c9d707376 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-04 |
| filingDate | 2005-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2011-02-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_8aeb0ea5e44d1cfd1c1239070fb4cbb0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d79e2904205b7e790b314b3a695f4b94 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ee9490bc8a558391f6f6fbc17e689c0f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bc8a31bebadcc6255382aa26d780e159 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d29ab52433e15f5ec498be32a6527efe http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_050b1b48bce653b68b33fe9dc5529bda http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2fd369404835afb9aaa909b7e0e6effe |
| publicationDate | 2011-02-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2352958-T3 |
| titleOfInvention | A PROCESS FOR THE PREPARATION OF IMATINIB BASE. |
| abstract | A process for the preparation of imatinib base and pharmaceutically acceptable acid addition salts thereof, which comprises: a) reacting 2-methyl-5-nitroaniline with cyanamide in the presence of concentrated hydrochloric acid to obtain 1- ( 2-methyl-5-nitrophenyl) -guanidine and convert said 1- (2-methyl-5-nitrophenyl) -guanidine hydrochloride into 1- (2-methyl-5-nitrophenyl) -guanidine nitrate; b) independently, the condensation of 3-acetylpyridine with N, N-dimethylformamide dimethyl acetal using a molar excess of 1.2-2.0 equivalents of said acetal per 1 mol of 3-acetylpyridine and while removing methanol in the course of the reaction by distillation , to obtain 3- (dimethylamino) -1- (3-pyridinyl) -prop-2-en-1-one; c) react 3- (dimethylamino) -1- (3-pyridinyl) -prop-2-en-1-one obtained in step b) without its purification with 1- (2-methyl-5- nitrophenyl) nitrate) - guanidine obtained in step a) to obtain N- (5-nitro-2-methylphenyl) -4- (3-pyridinyl) -2-pyridinamine; d) reduce the N- (5-nitro-2-methylphenyl) -4- (3-pyridinyl) -2-pyridinamine obtained in step c) to N- (5-amino-2- methylphenyl) -4- (3 -pyridinyl) -2-pyridinamine using hydrazine in the presence of Raney nickel, where hydrazine is present in the reaction medium in permanent excess; e) condensing N- (5-amino-2-methylphenyl) -4- (3-pyridinyl) -2-pyridinamine obtained in step d) with 4-chloromethylbenzoyl chloride in the presence of an inorganic base, diluting the mixture of react with water and isolate 4-chloromethyl-N- {[4- methyl-3- (4-pyridin-3-yl) pyrimidin-2-ylamino] -phenyl} -benzamide; f) condensing the 4-chloromethyl-N - {[4-methyl-3- (4-pyridin-3-yl) pyrimidin-2-ylamino] -phenyl} -benzamide obtained in step e) with N-methylpiperazine, in where Nmethylpiperazine is used in a molar excess of 2-12 equivalents with respect to 4-chloromethyl-N - {[4-methyl-3- (4-pyridin-3-yl) pyrimidin-2-ylamino] -phenyl} -benzamide ; g) dilute the reaction mixture with water or isopropanol or acetone, and optionally neutralize; h) isolate imatinib base precipitated in step g); and i) optionally, converting the imatinib base by a known method in its pharmaceutically acceptable acid addition salt. |
| priorityDate | 2004-12-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 112.