http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2010168433-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f7ddc4774cf5f8a0bda44a780d73c53d |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D401-12 |
| filingDate | 2008-06-05-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_de3e64715be9af8d71d7a55722bf9448 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c2b12d38f241af16ae170693f49cf577 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1ce2cdeb10874d7c7ef03e927e515c02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_64ed94b440aff659223a8f22d6dcc6ea http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_b0fa755ad4ac23fea9527f1ca8aaac1e http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_af5a88ae1dcefee065ed5668f48c874f |
| publicationDate | 2010-07-01-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | US-2010168433-A1 |
| titleOfInvention | Process for preparing bepotastine and intermediates used therein |
| abstract | A process for stereospecific preparation of bepotastine of formula (I) and novel intermediates used therein having formulae (II) to (IV) are provided. The inventive process comprises subjecting (RS)-4-[(4-chlorophenyl)(2-pyridyl)methoxy]piperidine to a reaction with a 4-halobutanoic acid l-menthyl ester, halo being chloro, bromo or iodo, in an organic solvent in the presence of a base to produce (RS)-bepotastine l-menthyl ester of formula (II), conducting a reaction of the compound of formula (II) with N-benzyloxycarbonyl L-aspartic acid in an organic solvent to induce selective precipitation of bepotastine l-menthyl ester.N-benzyloxycarbonyl L-aspartate of formula (III), filtering the precipitates formed in step 2) to isolate the compound of formula (III), treating the compound of formula (III) with a base to liberate bepotastine l-menthyl ester of formula (IV), and hydrolyzing the compound of formula (IV) in the presence of a base. The inventive process can provide bepotastine having a high optical purity of not less than 99.5% in a high yield, and thus, is useful in the development of anti-histamines and anti-allergic agents. |
| priorityDate | 2007-06-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 220.