| abstract |
FIELD: chemistry. n SUBSTANCE: invention relates to novel compounds of formula 10 and method for production thereof. Compounds possess properties of receptor tyrosine kinase type I inhibitors and can be used in treating hyperproliferative disorders. Invention also relates to novel intermediate compounds of formula 8 and 9 and to method of producing compounds 9. Compounds 10 and 8 correspond to common formulas (8) (10), where each R 6 , R 8 and R 8a are independently hydrogen or C 1 -C 6 alkyl, where said alkyl is optionally substituted OR 15 ; or R 8 and R 8a together with atom to which they are connected, three-six-Member carbocyclic ring is formed; and R 15 is hydrogen or C 1 -C 6 alkyl. Connection 9 corresponds to general formula (9), where A represents O; E represents , where X is CH; D 1 , D 2 and D 3 independently represent N or CR 19 ; D 4 and D 5 are independently N or CR 19 and D 6 represents O, S or NR 20 , at least one of D 4 and D 5 is not CR 19 ; D 7 , D 8 , D 9 and D 10 represent independently N or CR 19 , wherein at least one of D 7 , D 8 , D 9 and D 10 represents N; R 1 represents H or C 1 -C 6 alkyl; each R 2 independently represents halogen, cyano, trifluoromethyl, difluoromethyl, ftormetil or C 1 -C 6 alkyl; each R 6 , R 8 and R 8a are independently hydrogen or C 1 -C 6 alkyl, where said alkyl is optionally substituted by OR 15 , or R 8 and R 8a together with atom, to which they are bonded, 3-6-member carbocyclic ring is formed; R 15 represents H or C 1 -C 6 alkyl; each R 19 independently represents H, halogen or C 1 -C 6 alkyl; each R 20 is independently hydrogen or C 1 -C 4 alkyl, j is 0 and n represents 0, 1 or 2. n EFFECT: method of preparing compound of formula 10 involves condensation of compound of formula 8 with compound of formula 2 (2) in presence of acid in acceptable solvent, followed by thiourea of formula 9 cyclization, preferably in water solution of NaOH in tetrahydrofuran with addition of thozilchloride TsCl. n 9 cl, 1 tbl, 281 ex |