http://rdf.ncbi.nlm.nih.gov/pubchem/patent/KR-101404263-B1
Outgoing Links
| Predicate | Object |
|---|---|
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P11-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-26 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-26 |
| filingDate | 2008-01-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2014-06-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2014-06-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | KR-101404263-B1 |
| titleOfInvention | (1R) -2- (4-methoxyphenyl) -l-methylethyl] amino] ethyl] -2 (lH) -dihydroxy- Process for preparing quinolinone monohydrochloride |
| abstract | The present invention provides a process for the preparation of more convenient CHF4226 with a similar methodology, including the following step according to Scheme 1, instead of the process disclosed in EP 0147719.n n n (a) reacting a compound of formula (XII), wherein X is a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine, and R is a hydroxyl-protecting group, to obtain a compound of formula (XIII) '), Wherein R' is an amino-protecting group;n n n (b) reducing the compound to obtain a compound of formula (XIV) which already has the correct (R), (R) configuration;n n n (c) deprotecting compound (XIV) to obtain compound (I);n n n The (R), (R) diastereomeric selectivity of compound (XIV) is at least 60%, preferably at least 80%, even more preferably at least 90%, most preferably at least 95%.n n n Preferably, the (R), (R) diastereomeric selectivity is further increased by recrystallization of compound (I) and compound (XIV), more preferably by recrystallization of compound (XIV).n n n Preferably, the hydroxyl-protecting group R is selected from the group consisting of benzyl, p-methoxybenzyl, 3,4-dimethoxybenzyl, p- or o-nitrobenzyl, benzyloxycarbonyl and p-methoxybenzyloxycarbonyl Lt; RTI ID = 0.0 > phenyl < / RTI > lower alkyl. Preferably, the amino-protecting group R ' is a substituted or unsubstituted alkyl group selected from the group consisting of benzyl, p-methoxybenzyl, p-fluorobenzyl, p- chlorobenzyl, p- bromobenzyl, diphenylmethyl and naphthylmethyl Unsubstituted phenyl lower alkyl.n n n More preferably, R = R 'and even more preferably R and R' are benzyl groups.n n n In one preferred embodiment, the R and R 'protecting groups are simultaneously removed. In a more preferred embodiment, the deprotection is catalytic debenzylation.n n n The present invention further relates to the compound (XIII) and the compound (XIV) obtained as a stable intermediate of the above-mentioned reaction.n n n Quinolinone monohydrochloride, Tanabe, CHF4226 |
| priorityDate | 2007-01-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 50.