http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-035081-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6572ff5df928fd17340eb2a8cb6d8502 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D209-42 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-0222 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07K5-06026 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07K5-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07B61-00 |
filingDate | 2002-07-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_7240115990564141d9dc6f0f1ca9bb01 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_2fdcd08c184de339633ae9c65f211c07 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_64c1e44d2a4aabb2a4f1d654d460e607 |
publicationDate | 2004-04-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | AR-035081-A1 |
titleOfInvention | A NEW PROCEDURE FOR SYNTHESIS OF ACID COMPOUNDS OF (2S, 3AS, 7AS) -1 - [(S) -ALANIL] -OCTAHIDRO-1H-INDOL-2-CARBOXILICO AND APPLICATION IN THE SYNTHESIS OF PERINDOPRIL |
abstract | Industrial synthesis process of the compound of formula (1) where R1 represents a hydrogen atom or a linear or branched (C1-6) alkyl or benzyl group, and R2 represents a protective group of the amino function, because the ester is reacted of formula (2) where R1 is as defined in formula (1), with the alanine compound of formula (3) where R2 is as defined in formula (1), in an organic solvent such as, by for example, tetrahydrofuran or ethyl acetate, in the absence of 1-hydroxybenzotriazole or in the presence of an amount of 1-hydroxybenzotriazole less than 0.6 mol per mol of compound of formula (2) used, in the presence of an amount of dicyclohexylcarbodiimide between 1 and 1.2 mol per mole of compound of formula (2) used, and of an amount of triethylamine between 1 and 1.2 mol per mole of compound of formula (2) used, at a temperature between 20 ° and 50 ° C, to drive later for isolation and recrystallization to the compound of formula (4) where R1 and R2 are as defined above, which is hydrogenated in the presence of a catalyst such as, for example, Pd / C, Rh / C, Pt / C, Ni / C or PtO2, under a hydrogen pressure between 1 and 40 bars, at a temperature between 30 ° and 70 ° C, to lead to the compound of formula (1). Application in the synthesis of perindopril and its pharmaceutically acceptable salts. |
priorityDate | 2001-07-24-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 35.