http://rdf.ncbi.nlm.nih.gov/pubchem/patent/ES-2330102-T3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_89b60e340c7765626013119f28c35bfd |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K7-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K7-22 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K1-06 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K1-113 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K7-22 |
| filingDate | 2003-12-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2009-12-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e2a1408f93c29d1948a11603394c5bb8 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_405ab5851ff71494b1eb9cd9bd706f18 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_93e04ffc19be7486676cf4b94c41b295 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2c40529fa35baec1ff2f913b5fac0af7 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_502bec17bc7dd1318c97a3ffa667cc97 |
| publicationDate | 2009-12-04-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | ES-2330102-T3 |
| titleOfInvention | PROCESS FOR THE PREPARATION OF NEPADUTANT BICYCLE HEXAPEPTIDE. |
| abstract | Process for the preparation of bicyclic peptide compounds of formula (I) in liquid phase: ** (See formula) ** comprising the following steps: 1) deprotection of the linear pentapeptide of formula (II) in the presence of a solvent to obtain the compounds of formula (III): ** (See formula) ** in which A1 and A2 are two different nitrogen protecting groups, and R5 and R6, being different from each other, are chosen from the group consisting of benzyloxy groups and lower alkyloxy groups in which the alkyl part comprises a linear or branched C1-C4 group; 2) intramolecular cyclization of the compound of formula (III) from step 1) in the presence of a solvent and a suitable coupling agent giving rise to the compound of formula (IV) ** (See formula) ** in which R5 it is as defined above; 3) deprotection of the compound of formula (IV) from step 2) in the presence of a solvent giving rise to the compound of formula (V) ** (See formula) ** in which R5 is as defined above; 4) coupling between the compound of formula (V) from step 3) and a protected amino acid of formula (VIa) in the presence of a solvent, giving rise to compounds of formula (VII) ** (See formula) ** in that A3 is a nitrogen protecting group; R7 is selected from lower benzyloxy and alkyloxy groups, in which the alkyl part comprises a linear or branched C1-C4 group; R8 is a residual group derived from a carboxyl group activation procedure; 5) deprotection of the compound of formula (VII) from step 4) in the presence of a solvent giving rise to the compound of formula (VIII) ** (See formula) ** in which R7 is as defined above; 6) intramolecular cyclization in the presence of a solvent and a suitable coupling agent, of the compound of formula (VIII) from step 5) giving rise to a bicyclic compound of formula (IX) ** (See formula) ** in the that R7 is as defined above; 7) deprotection of the bicyclic compound of formula (IX) from step 6) in the presence of a solvent obtaining the compound of formula (I) ** (See formula) ** in which R7 is as defined above. |
| priorityDate | 2002-12-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 171.