http://rdf.ncbi.nlm.nih.gov/pubchem/patent/EP-0699673-B1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_2ca2e4410855da087e11bf3eea8933fa |
| classificationCPCAdditional | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D295-088 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D333-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07C229-38 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P5-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P19-10 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-092 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D295-08 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D333-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P19-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D207-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D409-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-195 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C217-54 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-4433 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-445 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C213-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C- http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07C217-22 |
| filingDate | 1995-08-30-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| grantDate | 1998-04-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_d59569b546900c44db9faa81fdc33d46 |
| publicationDate | 1998-04-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | EP-0699673-B1 |
| titleOfInvention | Process for preparing benzoic acid derivative intermediates and benzothiophene pharmaceutical agents |
| abstract | The present invention provides a novel process for preparing a compound of formula I <CHEM> wherein R is C1-C4 alkyl; R<1> and R<2> each are independently C1-C4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidino, dimethylpyrrolidino, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; and n is 2 or 3; or a pharmaceutically acceptable salt thereof, comprising a) condensing (C1-C4 alkyl) 4-hydroxybenzoate with ethylene carbonate or propylene carbonate in the presence of a condensation catalyst and a moderately polar, water immiscible solvent having a high boiling point; b) reacting the product of step a), a compound of formula III <CHEM> wherein R and n are as defined above, with a leaving group donor; and c) reacting the product of step b), a compound of formula IV <CHEM> wherein R and n are as defined above and X is a leaving group, with a base selected from the group consisting of piperidine, pyrrolidine, methylpyrrolidine, dimethylpyrrolidine, morpholine, dimethylamine, diethylamine, and 1-hexamethyleneimine. The product of the above process, a compound of formula I, also is novel and is useful for the preparation of pharmaceutically active compounds of formula II, particularly via the following novel process <CHEM> wherein R is C1-C4 alkyl; R<1> and R<2> each are independently C1-C4 alkyl, or combine to form piperidinyl, pyrrolidinyl, methylpyrrolidino, dimethylpyrrolidino, morpholino, dimethylamino, diethylamino, or 1-hexamethyleneimino; and n is 2 or 3; or a pharmaceutically acceptable salt thereof, comprising a) condensing (C1-C4 alkyl) 4-hydroxybenzoate with ethylene carbonate or propylene carbonate in the presence of a condensation catalyst and a moderately polar, water immiscible solvent having a high boiling point; b) reacting the product of step a), a compound of formula III <CHEM> wherein R and n are as defined above, with a leaving group donor; c) reacting the product of step b), a compound of formula IV <CHEM> wherein R and n are as defined above; and X is a leaving group, with a base selected from the group consisting of piperidine, pyrrolidine, methylpyrrolidine, dimethylpyrrolidine, morpholine, dimethylamine, diethylamine, and 1-hexamethyleneimine; d) reacting the product of step c) with a compound of formula IV <MATH> wherein R<3> and R<4> are as defined above, or a pharmaceutically acceptable salt thereof; e) optionally removing the reaction product from step d) ; and f) optionally forming a salt of the reaction product from either step d) or step e). |
| isCitedBy | http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6410587-B1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8158670-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6569441-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8097642-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6491938-B2 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6117911-A http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-6262079-B1 http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-8067022-B2 |
| priorityDate | 1994-08-31-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
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