http://rdf.ncbi.nlm.nih.gov/pubchem/patent/CZ-211499-A3
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_c7ad58d3c0b071069a8ee0cb8c8ba2e8 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D471-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-56 |
| classificationIPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-06 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D215-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D498-04 http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D471-04 |
| filingDate | 1999-06-11-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| inventor | http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_efe324052505f0419aa9d92b40877685 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_93a47b0229cf652dee2228b9cbf14d78 http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_ed1277485db93c36de28570fea687630 |
| publicationDate | 1999-12-15-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | CZ-211499-A3 |
| titleOfInvention | Process for preparing quinolocarboxylic acids and naphthyridonecarboxylic acids and their esters |
| abstract | Preparation of quinolone or naphthyridone 3-carboxylic acid derivatives (including esters) (I) from benzoyl or nicotinoyl chlorides (II), comprises: (a) reaction with aminoacrylate esters; (b) transamination; (c) cyclization; and optionally (d) saponification; are carried out using the same low polarity or non-polar solvent for stages (a)-(c), without isolation of intermediates. Preparation of quinolone or naphthyridone carboxylic acid derivatives of formula (I) involves: (a) reacting a benzoyl or nicotinoyl chloride of formula (II) with an aminoacrylic acid ester of formula Z1Z2N-CH=CH-COOR'1 (III) in presence of a base; (b) subjecting the obtained (hetero)aroyl-acrylate ester of formula (IV) to amine exchange reaction with an amine of formula Y-NH2 (V); (c) cyclizing the obtained (hetero)aroyl-acrylate ester of formula (VI) in the presence of base to give an ester (I; R1 = R'1); and optionally (d) saponifying and isolating the acid (I; R1 = H) after addition of an acid. The intermediates (IV) and (V) are not isolated, and steps (a)-(c) are carried out in the same low-polarity or non-polar solvent: R1 = H or R'1; R'1 = 1-4C alkyl; R2, R3, R6 = halo; R4 = H, halo or NO2; Y = 1-6C alkyl, 2-fluoroethyl, cyclopropyl, fluorocyclopropyl, isopropyl, 4-fluorophenyl or 2,4-difluorophenyl; A = N or CR5; R5 = H, Me, OMe, halo, NO2 or CN; or Y+R5 = -CH2CH2O- or -CH(Me)CH2O- (both bonded to N on the parent ring via C atoms); Z1, Z2 = 1-4C alkyl; or NZ1Z2 = saturated or unsaturated 5-6 membered ring, optionally containing 1 or 2 additional O, S or SO2 heteroatom(s). An Independent claim is included for the cyclization of (VI) to (I; R1 = R'1) in presence of base as a separate process, with the novel feature that reaction is carried out in a low polarity or non-polar solvent. |
| priorityDate | 1998-06-12-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
Incoming Links
Total number of triples: 113.