Patent RU-94041695-A (RU)
Inventor: VOL FGANG SHAPER
IPC: C07D239/46
Filed: 1993-03-10
Abstract: FIELD: organic chemistry. SUBSTANCE: product: derivatives of pyrimidine of the general formula (I)where: R- hydrogen, halogen, alkyl with 1-4 carbon atoms or cycloalkyl with 3-6 carbon atoms; R- hydrogen, alkyl with 1-4 carbon atoms, halogen, halogenalkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogenalkoxy with 1-4 carbon atoms, alkoxyalkyl with 1-4 carbon atoms in each alkyl moiety, alkylthio with 1-4 carbon atoms, alkylthioalkyl with 1-4 carbon atoms in each alkyl moiety, alkylamino with 1-4 carbon atoms or dialkylamino with 1-4 carbon atoms in each alkyl moiety; R- hydrogen, alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogenalkoxy with 1-4 carbon atoms, halogen, alkylthio with 1-4 carbon atoms, amino, alkylamino with 1-4 carbon atoms or dialkylamino with 1-4 carbon atoms in each alkyl moiety, or Rand Rtogether with carbon atoms with which they bound form unsaturated or 5- or 6-membered isocyclic ring that (in the case of 5-membered ring) has oxygen atom instead of group CHand can be substituted with 1, 2 or 3 similar or different radicals from group involving alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogenalkyl with 1-4 carbon atoms, halogenalkoxy with 1-4 carbon atoms and halogen, or can has sulfur atom instead of group CHand can be substituted with 1, 2 or 3 similar or different radicals from group involving alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogenalkyl with 1-4 carbon atoms and/or halogenalkoxy with 1-4 carbon atoms, or Rand Rtogether with carbon atoms with which they bound form 5-, 6- or 7-membered unsaturated isocyclic ring that can has sulfur atom instead of group CHand can be substituted with 1, 2 or 3 alkyl groups with 1-4 carbon atoms; X - group NH or oxygen; E - direct bond or directed or branched alkanediyl with 1-4 carbon atoms; Q - has value of radical Q, being Qmeans cycloalkyl group of the general formula (II)where: n = 2-7; Rand Rare similar or different and mean hydrogen, alkyl with 1-12 carbon atoms, cycloalkyl with 3-8 carbon atoms, cycloalkylalkyl with 3-8 carbon atoms in cycloalkyl moiety and 1-4 carbon atoms in alkyl moiety, alkoxy with 1-8 carbon atoms, cycloalkoxy with 3-8 carbon atoms, alkylhydroxyalkyl with 1-4 carbon atoms in alkoxyl moiety and 1-4 carbon atoms in alkyl moiety, cycloalkylalkoxy with 3-8 carbon atoms in cycloalkyl moiety and 1-4 carbon atoms in alkoxyl moiety, trialkylsilyl with 1-8 atoms in each alkyl moiety, dialkyl-(phenylalkyl)-silyl with 1-8 carbon atoms in each alkyl moiety and 1-4 carbon atoms in alkyl moiety near phenyl, dialkyl-halogenalkylsilyl with 1-8 carbon atoms in each alkyl moiety and 1-4 carbon atoms in halogenalkyl moiety, dimethylphenylsilyl, halogenalkyl with 1-4 carbon atoms, halogen, halogenalkoxy with 1-4 carbon atoms, heteroaryl, phenyl, phenylalkyl with 1-4 carnon atoms in alkyl moiety, benzylhydroxy, benzylhydroxyalkyl with 1-4 carbon atoms in alkyl moiety, benzylthio, phenylthio or phenoxy being phenyl rings in 7 latters radical are free or substituted with one or two similar or different residues from group involving alkyl, with 1-8 carbon atoms, cycloalkyl with 3-8 carbon atoms, halogenalkyl with 1-4 carbon atoms, halogen, dialkylamino with 1-4 carbon atoms in each alkyl moiety, alkylthio with 1-4 carbon atoms, alkoxy with 1-8 carbon atoms, halogenalkoxy with 1-4 carbon atoms, alkoxy-alkoxy with 1-4 carbon atoms in each alkyl moiety, group HC-O-[CH-CH-O-],, 2-(tetrahydro-2H-pyrane-2-ylhydroxy)-ethoxy, alkenyl with 2-8 carbon atoms, alkynyl with 2-8 carbon atoms, benzylhydroxy-group phenyl moiety of which can be mono- or di-substituted with similar or different residues taken from group involving alkyl with 1-4 carbon atoms, halogenalkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogenalkoxy with 1-4 carbon atoms and halogen, trialkylsilylmethoxy with 1-4 carbon atoms in each alkyl moiety, cycloalkyl-alkoxy with 3-8 carbon atoms in cycloalkyl moiety and 1-4 carbon atoms in alkoxyl moiety, 1,3-dioxolane-2-ylmethoxy, tetrahydrofuran-2-ylmethoxy or tetrahydro-2H-2-ylmethoxy being Rand Rcan not mean simultaneously hydrogen and in two adjacent substituents which are similar or different and taken from group involving alkyl with 1-8 carbon atoms and alkoxy with 1-8 carbon atoms, one carbon atom can be substituted with the combined bond C-C binding both substituents, or Rand Rtogether with cycloalkyl group form 3-8-membered spiro-cyclic fused system that can has oxygen or sulfur instead of one or two groups CH, or together with carbon atoms with which they bound form 5- or 6-membered isocycle; X - 2, 3 or 4 or Q has value Qbeing Qmeans group of the general formula (III)where: Rmeans group of the general formula Z-W where Z means direct bond, carbonyl or sulfonyl, and W - aryl and heteroaryl that are free or substituted with one or two similar or different substituents from group involving alkyl with 1-8 carbon atoms, cycloalkyl with 3-8 carbon atoms, trifluoromethyl, halogen, alkoxy with 1-4 carbon atoms, dialkylamino with 1-4 carbon atoms in each alkyl group and alkylthio with 1-4 carbon atoms, mixture of their isomers or separated isomers and their acid-additive salts. Another object of invention is an agent for struggle against pests containing at least one solid and/or liquid carrier, at least one pyrimidine derivative of above indicated formula (I), mixture of its isomers or separate isomer or its acid-additive salt taken at effective amount. Another object of invention is a method of struggle against pests by their treatment or their biotope with pyrimidine derivative of above given formula (I), mixture of their isomers or separate isomers or its acid-additive salt at effective consumption. EFFECT: improved method of synthesis.