| 摘要 |
FIELD: chemistry.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, Rand Rare independently hydrogen or C-Calkyl, where said alkyl is optionally substituted OR; or Rand Rtogether with atom to which they are connected, three-six-Member carbocyclic ring is formed; and Ris hydrogen or C-Calkyl. Connection 9 corresponds to general formula(9), where A represents O; E represents, where X is CH; D, Dand Dindependently represent N or CR; Dand Dare independently N or CRand Drepresents O, S or NR, at least one of Dand Dis not CR; D, D, Dand Drepresent independently N or CR, wherein at least one of D, D, Dand Drepresents N; Rrepresents H or C-Calkyl; each Rindependently represents halogen, cyano, trifluoromethyl, difluoromethyl, ftormetil or C-Calkyl; each R, Rand Rare independently hydrogen or C-Calkyl, where said alkyl is optionally substituted by OR, or Rand Rtogether with atom, to which they are bonded, 3-6-member carbocyclic ring is formed; Rrepresents H or C-Calkyl; each Rindependently represents H, halogen or C-Calkyl; each Ris independently hydrogen or C-Calkyl, j is 0 and n represents 0, 1 or 2.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.9 cl, 1 tbl, 281 ex |
