http://rdf.ncbi.nlm.nih.gov/pubchem/patent/PL-211161-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6572ff5df928fd17340eb2a8cb6d8502 |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61K38-00 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06026 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-42 |
| classificationIPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K38-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D209-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-02 |
| filingDate | 2004-06-28-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_f5c79ee99565f9ce4e0f3c7c073f9c14 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5a0c70dd32466b232c55b736c15671c3 |
| publicationDate | 2012-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | PL-211161-B1 |
| titleOfInvention | A method for producing perindopril and its pharmaceutically acceptable salts |
| abstract | Industrial synthesis of perindopril (I) involves: (a) reacting N-((S)-ethoxycarbonyl-1-butyl)-(S)-alanine (II) with a sulfinyl chloride (III); (b) reacting the obtained ethyl (2S)-2-((4S)-4-methyl-2-oxido-5-oxo-1,2,3-oxathiazolidin-3-yl)-pentanoate (IV) with a (2S)-2,3,4,5,6,7-hexahydro-1H-indole-2-carboxylic acid compound (V); and (c) catalytically hydrogenating the obtained (2S)-1-((2S)-2-((1S)-1-(ethoxycarbonyl)-butylamino)-propionyl)-2,3,4,5,6,7-hexahydro-1H-indole-2-carboxylic acid compound (VI) under a pressure of 1-30 bars. Industrial synthesis of perindopril of formula (I) or its salts involves: (a) reacting N-((S)-ethoxycarbonyl-1-butyl)-(S)-alanine of formula (II) with a sulfinyl chloride of formula Cl-S(O)-R1 (III); (b) reacting the obtained ethyl (2S)-2-((4S)-4-methyl-2-oxido-5-oxo-1,2,3-oxathiazolidin-3-yl)-pentanoate of formula (IV) with (2S)-2,3,4,5,6,7-hexahydro-1H-indole-2-carboxylic acid or its ester of formula (V) (or its mineral or organic acid addition salt); (c) hydrogenating the obtained (2S)-1-((2S)-2-((1S)-1-(ethoxycarbonyl)-butylamino)-propionyl)-2,3,4,5,6,7-hexahydro-1H-indole-2-carboxylic acid or ester of formula (VI) in presence of a catalyst (e.g. palladium, platinum, rhodium or nickel) under a pressure of 1-30 (preferably 1-10) bars to give (I) (if necessary after deprotection of the acid function); and (d) optionally converting (I) into a salt (specifically the tert. butylamine salt). R1 = imidazolyl, benzimidazolyl or tetrazolyl; R2 = H, benzyl or 1-6C alkyl. |
| priorityDate | 2003-06-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 71.