http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CN-103012231-B
Outgoing Links
| Predicate | Object |
|---|---|
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-40 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P1-04 |
| filingDate | 2012-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 2015-08-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2015-08-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CN-103012231-B |
| titleOfInvention | The preparation method and application of Glycopyrronium Bromide chiral enantiomer |
| abstract | The invention belongs to medical art, disclose a kind of (3S of muscarinic receptor antagonist racemic drugs Glycopyrronium Bromide, 2 ' S), (3S, 2 ' R), (3R, 2 ' R) and (3R, 2 ' S) preparation method of type four kinds of chiral monomers, with TYR methyl esters, (R)-α-phenylethylamine is resolution reagent, chemical resolution method is adopted to split racemization α-cyclopentyl amygdalic acid, obtained (S)-α-cyclopentyl amygdalic acid respectively, (R)-α-cyclopentyl amygdalic acid, chiral intermediate (S)/(R)-α-cyclopentyl methyl mandelate is obtained respectively after esterification.Respectively with L/D-oxysuccinic acid for raw material, adopt the approach of chiral synthesize, through condensation, carbonyl reduction, catalytic hydrogenation or the de-benzyl of transfer hydrogenation reduction, reduction hydrocarbonylation or haloalkane hydrocarbonylation, four-step reaction obtains another important chiral intermediate (S)/(R)-N-methyl-3-hydroxyl pyrrolidine altogether.Above chiral intermediate is again through transesterify, quaterisation obtained four kinds (3S, 2 ' S), (3S, 2 ' R), (3R, 2 ' R) and (3R, 2 ' S) type Glycopyrronium Bromide chiral monomer respectively.Result shows (3R, 2 ' S), and-Glycopyrronium Bromide has the strongest cholinergic antagonistic action. |
| priorityDate | 2012-12-14-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 85.