http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CA-2263692-A1
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_f2d3599fb8f8f479dba95ca9bb504884 |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D211-58 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D211-58 |
filingDate | 1997-10-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ce90784b64c9b58af217f3e49eaa0ac5 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_74e2ef73e0bb77fcfe96a310bc7bc3e0 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ffa1d255b18e03f81af541ef85793cec |
publicationDate | 1998-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | CA-2263692-A1 |
titleOfInvention | Synthesis of cisapride |
abstract | This invention concerns a new process of preparing cisapride, and the pharmaceutically acceptable acid addition salts thereof, by reductively aminating 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinone in the presence of benzylamine under hydrogen in a reaction-inert solvent, yielding 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine having a cis/trans ratio of about 93/7, which is enriched in the amount of cis-stereoisomer by converting it into its acid addition salt, by treatment with a suitable inorganic acid, in an appropriate solvent, subsequent crystallisation and conversion to its free base form by treatment with an appropriate base, yielding 1-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine having a cis/trans ratio of equal to or higher than 98/2. Subsequently, cis-[3-(4-fluorophenoxy)-propyl]-3-methoxy-4-piperidinamine is reacted with the mixed anhydride of 4-amino-5-chloro-2-methoxy-benzoic acid and ethyl chloroformate in a reaction-inert solvent yielding cisapride. |
priorityDate | 1996-10-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 27.