Synthesis of 1,2,4-substituted hexahydropyridazines and X-ray structural investigation of 4-hydroxyimino-2-methyl-1-phenethylhexahydropyridazine

A series of new 1,2,4-substituted hexahydropyridazines was prepared in order to evaluate qualitatively and quantitatively the role and influence of substituents on the biological activity of this system. An X-ray structural investigation of 4-hydroxyimino-2-methyl-1-phenethylhexahydropyridazine was performed. The compounds considered exhibit moderate local anesthetic, antihistaminic, and anticonvulsive activity.Translated fromIzvestiya Akademii Nauk. Seriya Khimicheskaya, No. 3, pp. 539–541, March, 1993.     

Structure of 4-anilinopiperidine analgesics. I. The structure of the 2:1 solvate of 1(e)-(2-phenethyl)-2(e),5(a)-dimethyl-4(e)-(N-propionylanilino)-piperidine bisulfate monohydrate with cyclohexanone

An x-ray diffraction structural analysis was carried out using Cu radiation with 2975 reflections, 64° to R=0.073 for the bisulfate of the major component of the narcotic analgesic, phenaridine (1-(2-phenethyl)2,5-dimethyl-4-(N-propionylanilino)-piperidine citrate). The crystals studied obtained from cyclohexanone are a double solvate containing 1/2 randomly disordered cyclohexanone molecule and one water molecule per formal salt unit. The unit cell parameters for the monoclinic crystals are as follows: a=15.231(2), b=14.946(2), c=13.070(2) Å, -104.23(1)°, space group P2₁/c, Z=4. The methyl groups in the compound studied occupy the 2-equatorial and 5-axial positions relative to the piperidine ring. Taking account of the equatorial positions of the substitutents at the 1- and 4-positions of the piperidine ring, the compound designated should be designated the rel-(1R,2R,4S,5R) isomer. The cation has an extended conformation with ordinary geometric parameters. The relative arrangement of the pharmacophoric groups in the cation (benzene rings A and F, piperidine ring D, and the amide fragment) is similar to that for the groups in T-shaped morphine-like molecules.Institute of Fine Organic Chemistry, Academy of Sciences of the Armenian SSR. Translated from Zhurnal Strukturnoi Khimii, Vol. 30, No. 5, pp. 102–107, September–October, 1989.     

The structure of 4-anilinopiperidine analgesics. III. The structure of the acid sulfate of 1(e)-(2-phenethyl)-2(e), 5(e)-dimethyl-4(e)-(N-propylylanilino) piperidine

Institute of Fine Organic Chemistry, Academy of Sciences of the Armenian SSR. Translated from Zhurnal Strukturnoi Khimii, Vol. 31, No. 2, pp. 141–145, March–April, 1990.     

Comparative investigation of the effect of heat and optical radiation on the structure of island metal films by optical fluctuation microscopy

Variations in the structural parameters of island sodium films on the quartz surface, caused by heating or exposure to optical radiation, are investigated by the optical method proposed earlier. A correct scheme of processing the measured data is developed. It is shown that to determine the structure parameters, the measurements of both the mean values and fluctuations of transmission and reflection coefficients of the film and of their correlator are required. It is also demonstrated that under a number of assumptions, it is possible to determine the character of the process of evaporation of islands and to reveal the evolution of the distribution function by using the data of measurements. It was found experimentally that variations in the structural parameters of a film during its evaporation caused by heating of the substrate or irradiation by light can noticeably differ. This fact is explained by a difference in the mechanisms of action of heating and irradiation on an island.     

Synthesis of 2-substituted 3-formyl-5-methoxy-tetrahydrofurans from 2,5-dimethoxytetrahydrofuryl-3-carbinols

The acid-catalyzed rearrangement of 2,5-dimethoxytetrahydrofuryl-3-carbinol, obtained from 2,5-dimethoxy-3-formyltetrahydrofuran, gave the 2-substituted 3-formyl-5-methoxytetrahydrofuran.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 164–166, February, 1991.     

Synthesis and properties of 1,4,9-triazaspiro[5,5]undecane and 3,7,11-triazaspiro[5,6]dodecane

Bromination of 1-methylpiperidine-4-carboxaldehyde gave 4-bromo-1-methylpiperidine-4-carboxaldehyde hydrobromide which was used to synthesize 1,4,9-triazaspiro[5,5]undecane and 3,7,11-triazaspiro[5,6]dodecane. Cyanoethylation and alkylation with various alkyl halides gave their mono- and di-substituted derivatives. The side chain nitrile group was reduced and the hydrazide was obtained from the ester analog.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 12, pp. 1673–1676, December, 1986.     

Satellite Transition of the Resonance Doublet of the Na Atom in a Mixture with CF4

JETP Letters - The excitation spectrum of the resonance luminescence of Na atoms in a mixture with CF4 exhibits a satellite transition corresponding to the simultaneous optical excitation of the...     

Structure of 4-anilinopiperidine analgesics. II. The structure of 1(e)-(2-phenethyl)-2(e),5(a)-dimethyl-4(e)-(N-propyionyl-anilino)piperidine

Institute of Fine Organic Chemistry, Academy of Sciences of the Armenian SSR. Translated from Zhurnal Strukturnoi Khimii, Vol. 30, No. 5, pp. 185–189, September–October, 1989.