http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-5892055-A
Outgoing Links
Predicate | Object |
---|---|
assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_01d6907e84c5ae66c7b305baeb3f3fcf |
classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D235-14 |
classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D235-14 |
filingDate | 1998-06-26-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
grantDate | 1999-04-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_342a5432a50bb184d5efc742ae300454 |
publicationDate | 1999-04-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
publicationNumber | US-5892055-A |
titleOfInvention | Preparation of mibefradil via an acetamide anion |
abstract | A method of preparing 2- 2-{ 3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl methoxyacetate comprises contacting 6-fluoro-1-isopropyl-3,4-dihydro-1H-naphthalen-2-one with the dianion of N- 3-(1H-benzimidazol-2-yl)propyl!-N-methylacetamide to form N- 3-(1H-benzirnidazol-2-yl) propyl!-2-(6-fluoro-2-hydroxy-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-yl)-N-methylacetamide, reducing this to 2- 2-{ 3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1,2,3,4-tetrahydronaphthalen-2-ol, and treating the 2- 2-{ 3-(1H-benzirnidazol-2-yl)propyl!methylarnino}ethyl!-6-fluoro-1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-ol with methoxyacetic acid or an activated derivative of methoxyacetic acid. The invention is particularly applicable to the preparation of mibefradil, (1S,2S)-2- 2-{ 3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-yl methoxyacetate, and its dihydrochloride salt. N- 3-(1H-Benzimidazol-2-yl)propyl!-N-methylacetamide, and the acetic acid solvate of 2- 2-{ 3-(1H-benzimidazol-2-yl)propyl!methylamino}ethyl!-6-fluoro-1-isopropyl-1, 2,3,4-tetrahydronaphthalen-2-ol dioxalate, are new. |
priorityDate | 1997-04-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 167.