The aminomethylation of arbutin followed by complexation with copper diacetate resulted in the synthesis of 1,3-oxazine derivatives of arbutin, as well as the chelate O,N-complex: 1-(β- D -glucopyranosyl-1-oxy)-3-(dimethylaminomethyl)-4-hydroxybenzene diacetate cuprate. In silico and in vitro assays of the synthesized compounds show that the 2-cupra-1,3-oxazine derivative of arbutin is an uncompetitive inhibitor of the α-amylase enzyme.

A series of bi- and trinuclear pyrrole derivatives was prepared by the 5 mol % ZrOCl 2 ·8H 2 O-catalyzed CH- sp 2 -aminomethylation reaction of pyrrole with bis(1,3-oxazacycloalk-3-yl)methanes. The reaction proceeds at the positions 2, 5 or 2 of pyrrole depending on the amount of aminomethylating reagents obtained from formaldehyde and α,ω-amino alcohols (2-aminoethan-1-ol, 3-aminopropan-1-ol, 4-aminobutan-1-ol). The aminomethylation reaction of indole with bis(1,3-oxazolidin-3-yl)methane proceeds at the position 3. In the case of carbazole, N -aminomethylation proceeds under these conditions.

Novel palladium(II) and platinum(II) heterocycles were synthesized based 1,2-bis(3,5-dimethylisoxazol-4-ylmethylsulfanyl)ethane. According to X-ray Crystallographic data in molecule there are two bonds between divalent sulfur atoms and metal atom S-Pd-S to form a five-membered palladacycle in the twist-conformation with trans orientation of isoxazole rings. The syn-anti-isomerization for the palladaheterocycle in the solution is observed. The activation energy ΔH≠, ΔS≠ and rate of reversible syn-anti-isomerization were established by the dynamic 1H NMR method and quantum-chemical calculations. Proposed mechanism of syn-anti-isomerization of palladacycle via an open-chain forms was offered. It was shown that metallaheterocycle - cis-S,S-dichloro 1,2-[di-(3,5-dimethylisoxazol-4-yl)methylsulfanyl]ethane palladium(II) is efficient catalyst in the amination reaction of allyl phenyl ether and Sonogashira reaction.

Catalytic aminomethylation of pyrrole and indole with N , N , N′ , N′ -tetramethylmethanediamine in the presence of 5 mol % of ZrOCl 2 ·8H 2 O proceeds selectively at the positions 2 , 5 of pyrrole and 1 , 3 of indole. Carbazole under the same conditions affords 3-formyl-9-aminomethyl derivative. The reaction in the presence of 5 mol % of K 2 CO 3 occurs as monoaminomethylation: for pyrrole at the position 2 , for indole at the position 3 , and for carbazole at the nitrogen atom of the substrate. Water-soluble 1,1′-(1 H -pyrrole-2,5-diyl)bis( N , N -dimethylmethanamine) exhibits a fungistatic activity with respect to phytopathogenic fungi Rhizoctonia solani .

24 organic compounds have been extracted from the sap of the freshly harvested plants of marjoram (Origanum vulgare L.). This plant is widespread throughout Russia but not sufficiently used. However, we found that the set of its compounds contains aromatic compounds, terpenoids, saturated alcohols and carboxylic acids. Among the identified compounds, there are substances important for pharmacy and perfume industry such as linalool and its derivatives, eugenol, menthenols. Essential oil of Origanum vulgare L. significantly differ from the oils of the other members of this species. To obtain the oil, we have harvested marjoram samples in Arkhangel district of the Republic of Bashkortostan. The compounds of marjoram essential oil has been analyzed with chromatomass-spectrometry. Kovac retention indices have been provided for all the studied compounds. The data obtained may be useful for complex use of green sources of Russia.

One-pot synthesis of 1,3,5-thiadiazine-4-thione, 5-acyl-1,3,5-thiadiazinane and 3,7-dithia-1,5-diaza-bicyclo[3.3.0]octane was carried out by multicomponent reaction of biologically active aminosubstituted (acetylsalicylic acid amide, thiosemicarbazide, thiourea, hydrozine) with formaldehyde and hydrogen sulfide. The structures of synthesized compounds have been established by the methods of spectroscopy IR, NMR 1H and 13C. The growth-promoting activity of the synthesized compounds on yeast Saccharomyces cerevisiae produces ethanol was found. Test compounds were evaluated in a dose of 0.1; 0.2; 0.5 mg/100 ml of wort. The control was carried out by counting the number of yeast cells using the camera Goriaev and microscope.

Cyclothiomethylation of o -phenylenediamine with CH 2 O and H 2 S gives rise to 1,2,4,5-tetrahydrobenzo[ d ][1,3,6]thiadiazepine and 1,2,6,7-tetrahydrobenzo[ f ][1,3,5,8]dithiadiazonine, whereas m -phenylenediamine forms benzothiaza macroheterocycles of various structure, comprising 4–8 molecules of the starting diamine, formaldehyde, and hydrogen sulfide. 4,4′-Diaminodiphenyls give bis(1,3,5-dithiazinanes), along with oligomeric hetero(N,S,O)atomic compounds.

Thiomethylation of carboxylic acid hydrazides with dimethylaminomethyl sulfides RSCH 2 NMe 2 yielded the corresponding N ′, N ′-bis(sulfanylmethyl)carbohydrazides. When bis-sulfides Me 2 NCH 2 S(CH 2 ) n SCH 2 NMe 2 ( n = 2–4) are used for thiomethylation, N -(acylamino)-substituted 1,5-dithia-3-azacycloalkanes are formed. These compounds can also be synthesized by CuCl 2 ·2H 2 O-catalyzed thiomethylation of carboxylic acid hydrazides with either CH 2 O and thiols or α,ω-alkanedithiols.

Cyclothiomethylation was performed of heterochain (O, S-S, NH) α,ω-diamines with formaldehyde and H2S in aqueous medium at 20–60°C to obtain new α,ω-bis(1,3,5-dithiazinanes). The cyclocondensation of N-(3-aminopropyl)butane-1,4-diamine (spermidine), formaldehyde, and H2S proceeds efficiently in the medium of BuOH-H2O at 0°C and leads to the formation of previously unknown O,S-containing macroheterocycle, 1,7-dioxa-3,5,9,11-tetrathiacyclododecane. A fungicidal activity was found in 5,5′-(3,6-dioxaoctane-1,8-diyl)bis-1,3,5-dithiazinane with respect to microscopic fungi affecting agriculture.

Efficient method was developed for thiols aminomethylation using N,N,N ′, N ′-tetra-methylmethanediamine in the presence of Sm and Fe salts. Aminosulfides were obtained in high yields and selectivity.

Efficient procedures have been developed for the synthesis of amino sulfides by aminomethylation of thiols with higher geminal diamines, thiomethylation of secondary amines with N,N-dimethylaminomethyl sulfides, and decyclization of 1,3,6-oxadithiepane or N-tert-butyl-1,5,3-dithiazepane with secondary amines in the presence of rare-earth and transition metals.

Chemoselectivity of multicomponent reaction of anilines with the CH 2 O-H 2 S thiomethylating mixture in the synthesis of N -aryl-substituted 1,3,5-dithiazinanes, 1,3,5-thiadiazinanes, and 1,5-dithia-3,7-diazacyclooctanes has been studied depending on the type and mutual arrangement of substituents in the starting anilines, ratio of reagents, temperature, and reaction time. Conformation of the synthesized heterocycles in crystal has been found by X-ray diffraction. Interconversion of the heterocycles showed stability of N -aryl-1,3,5-dithiazinanes.

A series of 5-acyl-1,3,5-dithiazinanes were synthesized by multicomponent heterocyclization of amides with formaldehyde (CH2O) and hydrogen sulfide (H2S) in the presence of BuONa. Among the synthesized compounds, 5-trifluoroacetyl-1,3,5-dithiazinane and 5-acetylsalicyloyl-1,3,5-dithiazinane exhibited anti-inflammatory activity comparable with that of aspirin.

Thiomethylation of para -toluidine and 4(5)-methyl-2-aminothiazoles was used to synthesize N,N ′-dithol-4-yl-1,3,5-thiadiazinane and N,N ′-[methylene-bis-(thiomethylene)]-bis-[4(5)-methyl-1,3-thiazole-2-amines]. A fungicidal and fungistatic effect toward some microscopic fungi, plant-disease-producing factor, was revealed for these compounds.

The cyclothiomethylation of carboxylic acid hydrazides RCONHNH2 (R = C5H4N, Ph, 2-MeOC6H4, or 4-HOC6H4CH2) with formaldehyde and H2S at 70 °C affords predominantly the corresponding N-(1,3,5-dithiazinan-5-yl)amides, whereas this reaction at 0–−50 °C gives a mixture of the latter compounds with 3-acyl-1,3,4-thiadiazolidines. N-(1,3,5-Dithiazinan-5-yl)-amides were selectively synthesized by the reaction of carboxylic acid hydrazides with formaldehyde and H2S in the presence of BuONa in BuOH.

A series of 5-acyl-1,3,5-dithiazinanes were synthesized by multicomponent heterocyclization of amides with formaldehyde (CH2O) and hydrogen sulfide (H2S) in the presence of BuONa. Among the compounds synthesized, 5-trifluoracetyl-1,3,5-dithiazinane and 5-acetylsalicyloyl-1,3,5-dithiazinane exhibited antiinflammatory activity comparable with that of aspirin.