Evaluation of cyclodextrin polymer as a disintegrating agent

Cyclodextrin polymer was compared to other well known disintegrants concerning the swelling properties /water uptake, moisture uptake, hydration capacity, sedimentation volume in water/. Its high disintegrating effect was proved in directly compressed tablets as well as in tablets made by wet granulation. A remarkable improvement in tablet properties was observed. Not only the disintegration of tablets and the dissolution of the drug was accelerated but also the hardness increased when CDP was used as disintegrant.     

New method for the preparation of O-carbamoyl derivatives in the 4-hydroxyaminoimidazolidin-2-one series

The corresponding 4-(O-carbamoylhydroxyamino)imidazolidin-2-ones were obtained by cyclization of O,N-dicarbamoyl derivatives of N-(3-oximino-2-methyl-2-butyl)- and N-(1-oximino-2-cyclohexyl)methylamines in alkaline media. It was shown that the carbamoylation of 1-methyl-4,5-tetramethylene-3-(3,4-dichlorophenyl)-4-hydroxy-aminoimidazolidin-2-one gives, respectively, an O- or N-carbamoyl derivative, depending on whether it is carried out in alkaline or neutral solutions.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 399–401, March, 1984.     

Characterization and TLC-Bioautographic Detection of Essential Oils from Some Thymus Taxa. Determination of the Activity of the Oils and their Components Against Plant Pathogenic Bacteria

JPC – Journal of Planar Chromatography – Modern TLC - The chemical composition of the oils of four thyme (Lamiaceae) chemotypes (Thymus vulgaris L., Thymus serpyllum L., Thymus x...     

Investigations into functionally substituted azines.

Reaction of 2-N-potassiocyanamino-4,6-bisisopropyl(dimethylamino)-sym-triazines with acid 1,2,2,2-tetrachloroethylamides leads to the formation of 2-N-cyano-N-(1-acylamino-2,2,2-trichloroethyl)amino-4,6-bisisopropyl(dimethylamino)-sym-triazines. Reaction with 1-hydroxy(methoxy)-2,2,2-trichloroethylamides of chloroacetic acid leads to 2-(2-imino-4-oxooxazolidin-1-yl)-4,6-bis(dimethylamino)-sym-triazine and its 1-methoxy-2,2,2-trichloroethyl derivative substituted at the position 3 of the oxazolidine ring.     

Synthesis and thermal decomposition of haloalkoxy-sym-triazines. 8. Synthesis and thermal decomposition of 2-methoxy(methylthio)-4-(2-chloroethylthio)-6-dialkylamino-sym-triazines

New 2-chloroethylthio derivatives of sym-triazine were obtained by the reaction of mercapto-sym-triazines and dichloroethane. It was established that these chlorides undergo cyclization to give 2-dialkylamino-4-oxo(thioxo)-4,5,6,7-tetrahydrothiazolo [1,2-a]-sym-triazines, the structure of which was confirmed by PMR and mass-spectral data, at moderate temperatures.See [7] for Communication 7.Translated f rom Khimiya Geterotsiklicheskikh Soedinenii, No. 9, pp. 1275–1278, September, 1981.     

Quaternization of tetrazoles under high pressure and establishment of the structures of quaternary tetrazolium salts by 13C NMR spectroscopy

The quaternization of 1- and 2-acetonyl-5-R-tetrazoles, as well as dimethyltetrazole, was accomplished under high pressure conditions (5000–14,000 kgf/cm²) by means of bromoacetone and methyl iodide and at atmospheric pressure and room temperature under the influence of methyl fluorosulfate. The structure of the salts were ascertained by ¹³C NMR spectroscopy, and the principles of the change in the chemical shifts and the spin-spin coupling constants during quaternization and protonation of the tetrazoles were studied.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 8, pp. 1118–1124, August, 1982.     

Methodology of using expert systems for structure elucidation of organic molecules by their spectra

Major axioms underlying structure elucidation of molecules by their characteristic spectral data are considered. The amount of information obtained by solving the problem on structure elucidation of molecules serves as a basis to evaluate the quality of solution. Conditions for computer-aided solution of problems using expert systems (ES) are analyzed. Reasons for incorrect or zero solutions and for inconsistencies leading to negative results are examined. The role of additional information as a necessary condition for correct solution is discussed. On the basis of this analysis, a general strategy for structure elucidation of molecules by their spectra using ES is suggested. The principal idea is to use the iteration method, gradually increasing the rigidity of constraints. Strategies named ARCHEOLOGIST and SCULPTOR are discussed. Examples are given. Russian Scientific Research Institute of Organic Synthesis. Translated fromZhurnal Strukturnoi Khimii, Vol. 36, No. 3, pp. 548–558, May–June, 1995. Translated by L. Smolina     

Crystal and molecular structure of hexacarbomethoxycyclopropane

A. N. Nesmeyanov Institute of Heteroorganic Compounds, Academy of Sciences of the USSR. N. D. Zelinskii Institute of Organic Chemistry, Academy of Sciences of the USSR. Translated from Zhurnal Strukturnoi Khimii, Vol. 30, No. 3, pp. 171–173, May–June, 1989.