http://rdf.ncbi.nlm.nih.gov/pubchem/patent/PL-401218-A1
Outgoing Links
Predicate | Object |
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assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_6728292a022c6c19233992ea183f2374 |
classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-66 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-99 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C12N9-76 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07F9-40 |
filingDate | 2012-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_bd3feb0220ec4a666461de52a0463c91 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3caab5ad5d5e72d72c61e29916b5580f http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_11ef9486b3fef8a5584362d0363dfec3 |
publicationDate | 2013-06-10-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | PL-401218-A1 |
titleOfInvention | Fluoroalkyl esters of 1-aminoalkane phosphonic acids and their derivatives, the method of obtaining fluoroalkyl esters of 1-aminoalkane phosphonic acids and their derivatives and the use of fluoroalkyl esters of 1-aminoalkane phosphonic acids and their derivatives |
abstract | The invention discloses fluoroalkyl esters of 1-aminoalkane phosphonic acids and their derivatives, of the general formula I, in which R is a substituent analogous to the side chain of natural and unnatural amino acids: alanine, valine, phenylalanine, leucine, isoleucine, methionine, norvaline, homophenylalanine or amino-aminomasinic acid; RF is a fluoroalkyl chain, preferably a group -CH2CF3, -CH2CF2CF2CF3 or -CH2CF2CF2H; Y is hydrogen, a benzyloxycarbonyl group or the Bip-Val-Pro dipeptide residue. In a variation of the method of obtaining fluoroalkyl esters of 1-aminoalkanephosphonic acids and their derivatives of the general formula I, in which R is a substituent analogous to the side chain of natural and unnatural amino acids: alanine, valine, phenylalanine, leucine, isoleucine, methionine, norvaline, homophenylalanine or ; RF is a fluoroalkyl chain, preferably a group -CH2CF3, -CH2CF2CF2CF3 or -CH2CF2CF2H; Y is hydrogen, a benzyloxycarbonyl group or the Bip-Val-Pro- dipeptide residue characterized by the fact that the tri (fluoroalkyl) phosphite obtained by the reaction of fluoroalcohol and phosphorus (III) chloride is subjected to amidoalkylation in glacial acetic acid using benzyl carbamate and the appropriate aldehyde from the group: acetaldehyde, propionic, isomasyl, phenylacetic, butyral, isovalerian, 2-methylbutyric, 3-phenylpropionic or S-methyl-propionic aldehydes, followed by the synthesis of hydrobromides of fluoroalkyl esters of 1-aminoalkanephosphonic acids, in which the benzyl protective group is unlocked (Cbz), and in the next step is reacted with the Boc-Val-Pro-OH dipeptide molecule in the presence of a coupling reagent. The invention also relates to the use of fluoroalkyl esters of 1-aminoalkanephosphonic acids and their derivatives of general formula I as serine inhibitors of the chymotrypsin and elastase proteases. |
priorityDate | 2012-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
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Total number of triples: 55.