http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-2885276-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_966a6c1f382ec9bcb5e3839dfd73e5b8 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D231-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C281-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C227-16 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C271-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C269-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C281-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D231-14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C281-04 |
| filingDate | 2013-08-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_fec48dbe44a05f0f0c3b39b8934bdb03 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_94db340f489be26a21d28a776465b728 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_423391ae9c312a6da87d7a66e0bc7311 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_cfd6f3be84acc8c9216bb58988509c03 |
| publicationDate | 2015-06-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-2885276-A1 |
| titleOfInvention | Process for the preparation of pyrazole carboxylic acid derivatives |
| abstract | The present invention relates to a novel process for the preparation of a pyrazole carboxylic acid derivative of the formula (I) wherein R1 is C1-7-alkyl and R3 is C1-7-alkyl which is optionally substituted with halogen or C1-4-alkoxy. The pyrazole carboxylic acid derivative of the formula I can be used as building block in the preparation of pharmaceutically active principles, e.g. for compounds acting as phosphodiesterase (PDE) inhibitors, particularly PDE10 inhibitors. PDE10 inhibitors have the potential to treat psychotic disorders like schizophrenia (Int. Patent Publication WO 2011/117264). A synthetic approach to the pyrazole carboxylic acid derivative of the formula I has been described in scheme 3 of the Int. Patent Publication WO 2011/117264 applying a method disclosed in Hanzlowsky et al, J. Heterocyclic Chem. 2003, 40(3), 487-489. However, under the acid-catalyzed cyclocondensation conditions described, besides of the desired isomer, also a substantial amount of the undesired N-1 substituted isomer was formed. In many cases, especially on larger scale, this undesired isomer is the major product in the reaction mixture with ratios of up to 70:30 in favor of the undesired isomer, leading to isolated yields of ca. 30% of the undesired isomer, along with ca. 25% of the desired isomer. |
| priorityDate | 2012-08-17-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 175.