http://rdf.ncbi.nlm.nih.gov/pubchem/patent/AR-061098-A1
Outgoing Links
| Predicate | Object |
|---|---|
| assignee | http://rdf.ncbi.nlm.nih.gov/pubchem/patentassignee/MD5_24e76490bed88751680a5fef9bc73892 |
| classificationCPCInventive | http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D215-56 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P35-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/A61P43-00 http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D401-12 |
| filingDate | 2007-05-22-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationDate | 2008-08-06-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| publicationNumber | AR-061098-A1 |
| titleOfInvention | METHOD FOR PREPARING INTERMEDIATE QUINOLINE COMPOUNDS 4- HALOGENADA |
| abstract | Claim 1: A method of preparing a compound of formula (1) comprising the step of reacting a compound of formula (2) with a reagent of formula POX3 in the presence of a silica gel at a temperature greater than about 75 ° C , where X is halo, PG is a protective group selected from the group consisting of acyl, CH3OC (O) -, EtOC (O) -, Fmoc, trifluoroacetamide, Troc, Phenoc, benzamide, Teoc and cyclic imides; A is O, NR, or S; R is H, alkyl, alkenyl or alkynyl; and G, R1 and R4 are each independently hydrogen, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C2-6 alkenyloxy, C2-6 alkynyloxy, hydroxymethyl, halomethyl, C1-6 alkanoyloxy, C3-8 alkenyloxy, C3-8 alkynyloxy, C2-7 alkanoyloxymethyl, C4-9 alkenyloxymethyl, C4-9 alkyloxymethyl, C2-7 alkoxymethyl, C1-6 alkoxy, C1-6 alkylthio, C1-6 alkylsulfinyl, C1-6 alkylsulfonyl, C1-6 alkylsulfonamido, C2-6 alkenylsulfonamido, C2-6 alkynylsulfonamido, hydroxy, trifluoromethyl, trifluoromethoxy, cyano, nitro, carboxy, carboalkoxy C2-7, carboalkyl C2-7, phenoxy, phthalimide, phenyl, thiophenoxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzyloxy, benzylamino , C1-4 alkoxyamino, C1-6 alkylamino, C2-12 dialkylamino, N-alkylcarbamoyl, N, N-dialkylcarbamoyl, N-C4-12 alkyl-N-alkenylamino, N, N-C6-12 dialkylamino, phenylamino, benzylamino, formulas (3), R7- (C (R6) 2) gY-, R7- (C (R6) 2) pM- (C (R6) 2) kY-, or Het- (C (R6) 2) qW ( C (R6) 2-Y-; or R1 and R4 are as defined above and G is R2-NH-; or in case that any of the substituents R1, R4 or G were located on adjacent carbon atoms then they can be taken together as the divalent radical -O-C (R6) 2-O; Y is a divalent radical selected from the group consisting of - (CH2) a-, -O- and -NR6-; R7 is -NR6R6, -OR6, -J, -N (R6) 3+, or -NR6 (OR6), M is> NR6, -O-,> N- (C (R6) 2) pNR6R6, or> N - (C (R6) 2) p-OR6, W is> NR6, -O- or is a bond; Het is selected from the group consisting of morpholine, thiomorpholine, thiomorpholine S-oxide, S, thiomorpholine S-dioxide, piperidine, pyrrolidine, aziridine, pyridine, imidazole, 1,2,3-triazole, 1,2,4-triazole , thiazol, thiazolidine, tetrazol, piperazine, furan, thiophene, tetrahydrothiophene, tetrahydrofuran, dioxane, 1,3-dioxolane, tetrahydropyran, and the compound of formula (4) where Het is optionally mono- or di-substituted on carbon or nitrogen with R6, optionally mono- or di-substituted on the carbon with hydroxy, -N (R6) 2, or -OR6, optionally mono- or di-substituted on the carbon with the monovalent radicals - (C (R6) 2) s , OR6 or - (C (R6) 2) s N (R6) 2, and optionally mono or disubstituted on a carbon saturated with divalent radicals -O- or -O (C (R6) 2) sO-; R6 is hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-6 cycloalkyl, C2-7 carboalkyl, C2-7 carboxyalkyl, phenyl, or phenyl optionally substituted with one or more halogen, C1-6 alkoxy , trifluoromethyl, amino, C1-3 alkylamino, C2-6 dialkylamino, nitro, cyano, azido, halomethyl, C2-7 alkoxymethyl, C2-7 alkanoyloxymethyl, C1-6 alkylthio, hydroxy, carboxyl, C2-7 carboalkoxy, phenoxy, phenyl , thiophenoxy, benzoyl, benzyl, phenylamino, benzylamino, C 1-6 alkanoylamino, or C 1-6 alkyl; with the proviso that the alkenyl or alkynyl portion is attached to a nitrogen or oxygen atom through a saturated carbon atom; R2 is selected from the group consisting of formulas (5), R3 is independently hydrogen, C1-6 alkyl, carboxy, C1-6 carboalkoxy, phenyl, C2-7 carboalkyl, formula (6), R7- (C (R6) 2) s-, R7- (C (R6) 2) pM- (C (R6) 2) r-, R8R9-CH-M- (C (R6) 2) r-, or Het- (C (R6) 2) qW- (C (R6) 2) r-; R5 is independently hydrogen, C1-6 alkyl, carboxy, C1-6 carboalkoxy, C2-7 phenylcarboalkyl, formula (6), R7- (C (R6) 2) s-, R7- (C (R6) 2) pM- (C (R6) 2) r-, R8R9-CH-M- (C (R6) 2) r-, or Het- (C (R6) 2) qW- (C (R6) 2) r-; R8 and R9 are each independently - (C (R6) 2) rNR6R6, or - (C (R6) 2) rOR6; J is independently hydrogen, chlorine, fluorine, or bromine; Q is a C1-6 alkyl or hydrogen; a is 0 or 1; g is 1-6; k is 0-4; n is 0-1; m is 0-3; p is 2-4; q is 0-4; r is 1-4; s is 1-6; u is 0-4 and v is 0-4, where the sum of u + v is 2-4; x is 0-3; y is 0-1; z is 0-3; or its salt |
| priorityDate | 2006-05-23-04:00^^<http://www.w3.org/2001/XMLSchema#date> |
| type | http://data.epo.org/linked-data/def/patent/Publication |
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