Patent RU-94028278-A (RU)
Inventor: ARMIN KHEKEL
IPC: A61K31/495
Filed: 1994-08-01
Abstract: FIELD: organic chemistry. SUBSTANCE: product: derivatives of pyrimido-[5,4-d] -pyrimidine of the general formula (I)where: R- pyrrolidine-, piperidine- or hexamethyleneimino-group being one methylene-group in pyrrolidine-group at position 3, or in piperidine- and hexamethyleneimino-group at position 3 or 4 were substituted with group >CR-A-(RNR) where A means carbon-nitrogen bond or alkylene group with 1-3 carbon atoms; R- hydrogen atom, free alkyl group with 1-3 carbon atoms or that substituted with phenyl, and R- hydrogen atom or alkyl-group with 1-4 carbon atoms that is free or substituted with phenyl that is free or mono- or disubstituted with similar or different substituents taken from the group involving fluorine, chlorine or bromine atom, alkyl and alkoxyl-group correspondingly with 1-3 carbon atoms, alkyl-group with 1-4 carbon atoms substituted with carboxyl, alkylhydroxycarbonyl with 1-3 carbon atoms in alkoxyl moiety, cyano, aminocarbonyl, alkylaminocarbonyl with 1-3 carbon atoms in alkyl moiety, dialkylaminocarbonyl with 1-3 carbon atoms in each alkyl-group or two phenyl-groups, alkyl-group with 2-4 carbon atoms that is free or substituted at position 2,3 or 4 with hydroxyl, amino, alkyl- or dialkylamino-group with 1-3 carbon atoms in each alkyl moiety, or alkoxycarbonyl-group with total carbon atoms 2-4; or Rand Rtogether with nitrogen atom form cycloalkyleneimino-group with 3-7 ring members, morpholino-, thiomorpholino-, 1-oxido-thiomorpholino- or 1,1-dioxido-thiomorpholino-group, group >CO or >RO-C-ORwhere Rand Rare similar or different and mean alkyl-group with 1-3 carbon atoms; or Rand Rtogether form n-alkylene group with 2 or 3 carbon atoms, or group of the formulawhere Rmeans hydrogen atom or alkyl-group with 1-3 carbon atoms; R- hydrogen atom, alkyl-group with 1-3 carbon atoms or phenyl; Rand R, are similar or different and mean cyclic alkyleneimino- or alkenyleneimino-group with 5-7 ring members where through positions 2 and 3 or 3 and 4 1,4-butadienyl-bridge can be linked that can be mono-substituted with methylenedihydroxy-group or mono-, di- or tri-substituted with similar or different substituents from group involving fluorine, chlorine or bromine atoms, alkyl with 1-3 carbon atoms, alkoxyl with 1-3 carbon atoms, amino, alkylamino with 1-3 carbon atoms, dialkylamino with 1-3 carbon atoms in each alkyl moiety and alkanoylamino with 1-3 carbon atoms, morpholino-, thiomorpholino-, 1-oxidothiomorpholino-, 1,1-dioxidothiomorpholino-group or group RNR, where Rmeans hydrogen atom or alkyl-group with 1-4 carbon atoms that is free or substituted with carboxyl, cyano, alkoxycarbonyl with 1-3 carbon atoms in alkyl moiety or phenyl that is free or mono- or disubstituted with similar or different substituents from the group involving fluorine, chlorine or bromine atom, alkyl and alkoxyl-groups, respectively, with 1-3 carbon atoms, or at position 2,3 or 4 with amino-group, alkyl- or dialkylamino-group with 1-3 carbon atoms in each alkyl moiety, alkanoylamino-group with 1-3 carbon atoms, benzoylamino- or phenylsulfonylamino-group phenyl nucleus of which can be mono- or disubstituted with similar or different substituents from the group involving fluorine, chlorine or bromine atoms, alkyl and alkanoyl groups with 1-3 carbon atoms; R- hydrogen atom, alkyl-group with 1-4 carbon atoms that is free or substituted with phenyl or naphthyl, mono- or disubstituted similar or different substituents from the group involving fluorine, chlorine or bromine atoms, alkyl with 1-3 carbon atoms, alkoxyl with 1-3 carbon atoms, amino, alkyl- or dialkylamino-group with 1-3 carbon atoms in each alkyl moiety, alkanoylamino-group with 1-5 carbon atoms or anthracenyl-group being Rcan means free alkoxyl or alkylthio-group with 1-3 carbon atoms or that substituted with phenyl, and their salts. EFFECT: improved method of synthesis.