http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-038267-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c76ecadad74a1a35270b3e3a34d60f37 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P13-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P25-02 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P27-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P3-10 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P9-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P25-02 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D405-12 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61K31-501 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/A61P13-12 |
| filingDate | 2003-01-07-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2005-01-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-038267-A1 |
| titleOfInvention | PROCEDURE AND INTERMEDIATES FOR ANTIDIABETIC AGENTS OF PIRIDAZINONA |
| abstract | These compounds are pyridazinone aldose reductase inhibitors and are useful in the prevention and / or treatment of diabetic complications such as diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, diabetic cardiomyopathy, diabetic microangiopathy and diabetic macroangiopathy in mammals. It also refers to intermediates useful in the preparation of said aldose reductase inhibitors. Claim 1: A process for preparing a compound of formula (1), wherein: R1 and R2 are each independently hydrogen or methyl; and R3, R4, R5 and R6 are each independently H, halo, formyl, (C1-6) alkyl optionally substituted with up to three fluoro, (C1-6) alkoxy optionally substituted with up to fluoro, (C1-6) alkoxycarbonyl , (C1-6) alkyl enyloxycarbonyl, (C1-4) alkoxy (C1-4) alkyl, alkyl (C1-4) carbonylamide, cycloalkyl (C3-7) carbonylamide, phenylcarbonylamide, benzyl, phenyl or naphthyl, said benzyl being, phenyl and naphthyl optionally independently substituted with up to two substituents independently selected from halo, (C 1-6) alkyl optionally substituted with up to three fluoro, (C 1-6) alkoxy optionally substituted with up to three fluoro and (C 1-4) alkoxy -4); characterized in that it comprises the consecutive steps of: (a) reacting a compound of formula (2), in which R3, R4, R5 and R6 are each independently as defined above, with an organolithium compound in the presence of a source sulfur in a first inert reaction solvent, to form the reactive intermediate of formula (3); (b) reacting said reactive intermediate (3) with a compound of formula (4), to form a compound of formula (5); (c) reacting said compound of formula (5) with an alkaline (C1-2) alkoxide in an alkanol (C1-2), to form an ether compound of formula (6), wherein AIk is (C1-) alkyl 2); (d) reacting said compound of formula (6) with a mineral acid, to form a compound of formula (7); and (e) oxidizing said compound of formula (7) in a second inert reaction solvent, to form a compound of formula (1). |
| priorityDate | 2002-01-09-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 39.