http://rdf.ncbi.nlm.nih.gov/pubchem/patent/RU-2323214-C2

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filingDate 2004-06-14-04:00^^<http://www.w3.org/2001/XMLSchema#date>
grantDate 2008-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_6ac84770d7078e0be3868c15e829f619
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_e3c789f5e1acdfc6e715e0e5bbfbe7dc
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_c8e2e7fc4fbe5b2143b7394757bf2582
publicationDate 2008-04-27-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber RU-2323214-C2
titleOfInvention Methods for preparing derivatives of 1-[2-(benzimidazol-1-yl)quinolin-8-yl]piperidin-4-ylamine
abstract FIELD: organic chemistry, chemical technology, medicine, oncology, pharmacy. n SUBSTANCE: invention relates to a method for synthesis of compound of the formula (I): or its pharmaceutically acceptable salt, ether, ester, amide, hydrate or solvate wherein each R 1 , R 2 and R 3 is chosen independently from group consisting of hydrogen atom (H), (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl, halogen atom, cyano, -CF 3 , difluoromethoxy, trifluoromethoxy, -O-(C 1 -C 6 )-alkyl, -O-(C 3 -C 6 )-cycloalkyl and -NR 12 R 13 ; wherein R 4 represents -(CR 5 R 6 ) m H or -(CR 7 R 8 ) n (4-10-membered) aromatic or nonaromatic heterocycle comprising one or more heteroatoms each of them is chosen from oxygen (O), sulfurs (S) and nitrogen (N) atoms, and wherein m represents a whole number in the range from 1 to 5, and wherein n represents a whole number in the range from 0 to 5, wherein indicated 4-10-membered aromatic heterocycle is substituted possibly with 1-3 substitutes R 9 , and wherein indicated 4-10-membered nonaromatic heterocycle is substituted possibly with 1-3 substitutes R 10 by any position and substituted possibly with 1-3 substitutes R 11 by any position but not adjacent or directly bound to heteroatom; wherein Each R 5 , R 6 , R 7 and R 8 is chosen independently from group consisting of H and (C 1 -C 6 )-alkyl; wherein each R 9 is chosen independently from H, (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl, cyano, -CF 3 , difluoromethoxy, trifluoromethoxy, -O-(C 1 -C 6 )-alkyl, -O-(C 3 -C 6 )-cycloalkyl and -NR 14 R 15 ; wherein each R 10 is chosen independently from H, (C 1 -C 6 )-alkyl and (C 3 -C 6 )-cycloalkyl; wherein each R 11 is chosen from halogen atom, cyano, -CF 3 , difluoromethoxy, trifluoromethoxy, -O-(C 1 -C 6 )-alkyl, -O-(C 3 -C 6 )-cycloalkyl and -NR 16 R 17 ; wherein R 12 , R 13 , R 14 , R 15 , R 16 and R 17 are chosen independently from group consisting of H, (C 1 -C 6 )-alkyl and (C 3 -C 6 )-cycloalkyl wherein each abovementioned (C 1 -C 6 )-alkyl, (C 3 -C 6 )-cycloalkyl, -O-(C 1 -C 6 )-alkyl and -O-(C 3 -C 6 )-cycloalkyl substitutes wherein they present can be substituted independently with substitutes in the amount from 1 to 3 and chosen independently from group consisting of halogen atom, cyano, amino, (C 1 -C 6 )-alkylamino, [(C 1 -C 6 )-alkyl]-amino, perhalogen-(C 1 -C 6 )-alkyl, perhalogen-(C 1 -C 6 )-alkoxy, (C 1 -C 6 )-alkyl, (C 2 -C 6 )-alkenyl, (C 2 -C 6 )-alkynyl, hydroxy and (C 1 -C 6 )-alkoxy. Method of synthesis involves interaction of compound of the formula (II): wherein BOC represents tert.-butoxycarbonyl, and R 1 , R 2 , R 3 and R 4 are given above for compound of the formula (I) with metal alkoxide in the presence of water to obtain compounds of the formula (I). Invention provides a novel method for synthesis of compounds of the formula (I) that are useful in treatment of cells anomalous growth, such as cancer, in mammals. n EFFECT: improved method of synthesis, valuable medicinal properties of compounds. n 12 cl, 7 ex
priorityDate 2003-06-24-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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