The reaction of aromatic aldehydes with malononitrile, ethyl or butyl cyanoacetate and acetylacetone in the presence of NaOH under mild conditions (EtOH, 25°C) led to the formation of new series of (1S,5R,6R,9R)/(1R,5S,6S,9S)-2-amino-6,9-diaryl-7-acetyl-8-methyl-4-oxo-5-cyano-3-azabicyclo[3.3.1]nona-2,7-diene-1-carboxylic acids esters. A plausible mechanism of the cascade reaction was proposed.

The sequential reaction of furfural with cyclic secondary amines and further with benzaldehyde and cyanoacetates affords new 2,4-dicyano-8-(R2N)-6-oxo-3-phenylbicyclo[3.2.1]-octane-2,4-dicarboxylates as rac-(1R,2R,3R,4S,5S,8R)-diastereomers. The structures of the reaction products were determined by X-ray diffraction.

Наука России: Цели и задачи «Силиплантом» отличается наибольшими таксационными показателями, но с сильной вариативностью значений.*** 1. Чукарина А.В.Совершенствование технологии выращивания посадочного материала сосны в питомниках степного Придонья (на примере Ростовской области) //Автореферат диссертации на соискание ученой степени.

Cascade reaction of 2 equiv. of furfural (or equimolar amounts of furfural and aromatic aldehyde) with secondary amines and ethyl cyanoacetate afforded diethyl esters of 8-(dialkylamino)-3-aryl-6-oxo-2,4-dicyanobicyclo[3.2.1]octane-2,4-dicarboxylic acids with yields of 37–54%. Antimicrobial activity of a number of obtained compounds in vitro was studied, and biological activity in silico was analyzed. The obtained bicyclo[3.2.1]octanes are inactive or exhibit weak fungicidal activity, but exhibit moderate bactericidal effect.

The reaction of 5-acetyl-4-aryl-6-hydroxy-3,6-dimethyl-4,5,6,7-tetrahydroindazoles p-toluenesulfonyl chloride in boiling acetone in the presence of triethylamine was found to occur in a completely regioselective with the exclusive formation of 5-acetyl-4-aryl-6-hydroxy-3,6-dimethyl-1-(4-methylbenzenesulfonyl)-4,5,6,7-tetrahydroindazoles. The experimental results were confirmed by quantum chemical calculations. In silico biological activity evaluation of the synthesized compounds was performed.

As a result of the studies, a new multicomponent condensation of dime-done, aromatic aldehydes, acetoacetic ester and allylamine in amolar ratio of 1: 2: 1: 1, respectively, was revealed. These reactions lead to the formation of ethyl-3-(allylamino)-9,9-dimethyl-7,11-dioxo-1,5diarylspiro[5.5]undec-2-en-2-car-boxylates. Thus, new possibilities of multicomponent reactions involving 1,3-dicarbonyl compounds proceeding via the cascade carbocyclization mechanism are shown. Structure of all synthesized compounds confirmed by modern physical methods of analysis. By the method of XRD analysis the stereo orientation of substituents in the spirocyclic framework is established.

As a result of triple condensation of malonodinitrile with benzaldehyde and ethyl 2-chloro-3-oxobutanoate a compound with 3-azabicyclo[3.1.0]hexane framework is formed whose crystal structure is determined by X-ray crystallography. In the crystal structure a layered character of the molecular packing is found. Molecules are linked in the layer by H bonds of N-H…O=C and C-H…O=C types and also a large number of atom-atom contacts whose energy corresponds to potential wells.

On the base of 3-nitrobenzaldehyde and acetylacetone 2,4-diacetyl-3-(3'-nitrophenyl)-5hydroxy-5-methylcyclohexanone was synthesized. The crystal structure of the reagent was set by XRD. The crystals are triclinic: a=8,1300(8), b=8,8135(9), c=13,6189(14) Å, α=99,088(2)°, β=92,825(2)°, γ=104,969(2)°, V=926,74(16) Å, space group, P21/m, Z=2. XRD results showed that the crystal structure of the reagent corresponds to enol form. The complexation of the reagent with iron (III) ions in the presence of 1,10-phenanthroline investigated and highly selective method of determination for the direct determination of trace iron in the strawberry and apricot developed.

Three-component condensation reaction of malonodinitrile, 4-chloro-benzaldehyde and ethyl 4-chloro-3-oxobutanoate has been analyzed to establish that in the presence of NaOH base, the reaction proceeds by Knoevenagel-Michael-Perkin cascade carbocyclization to form ethyl-1-acetyl-3-(4-chlorophenyl)-2,2-dicyanocyclopropane carboxylate. The structure of the reaction product examined through with X-ray analysis.

In the world, there are currently has developed a quite difficult situation with the use of antibiotics in infectious diseases treatment. According to the fact, clinical isolates of the bacteria resistant against most of antibiotics in many cases. The treatment of diseases, caused by even opportunistic strains such as S. aureus, E. coli, etc., becomes more difficult. Antibiotics are used strictly for a purpose with a certain doze and duration in order to prevent the emergence and spread of resistance. For example, in the treatment of intestinal infections, antibiotic treatment is justified only in 20% of cases. Another serious problem with some antibiotics - is their low bioavailability (for instance, tsefeksim - 40-50% of bioavailability) and high toxicity (fluoroquinolones -hepatotoxicity, nephrotoxicity and ototoxicity).

The reaction of 2,4-diacetyl-5-hydroxy-5-methyl-3-phenylcyclohexanone-1 with phenylhydrazine is conducted, and the crystal structures of its products, 1-(6-hydroxy-3,6-dimethyl)-2,4-diphenyl-4,5,6,7-tetrahydro-2H-indazol-5-yl)ethane-1-one and 1-(2-hydroxy-2-methyl-6-phenyl-4-(2-phenylhydrazono)-5-(1-(2-henylhydrazono)ethyl)cyclohexyl)ethane-1-one, are determined by single crystal XRD.

The reaction of diethyl-5-methyl-3-oxo-1,2,3,6-tetrahydro-[1,1′-diphenyl]-2,6-dicarboxylate with (1-(4-bromophenyl)ethylidene)hydrazine is conducted, and the crystal structure of the product of this reaction (diethyl-5-(2-(1-(4-bromophenyl)ethylidene)hydrazinyl)-3-methyl-1,2-dihydro-[1,1′-diphenyl]-2,6-dicarboxylate) is determined by single crystal X-ray diffraction. The conformation of the cyclohexadiene ring in the form of a strongly distorted half-chair is determined based on the X-ray diffraction data. The presence of the intramolecular hydrogen bond of the N–H…O=C type is noted.