The first synthesis of nitro-substituted cyclopropanes and spiropentanes via oxidation of the corresponding amino derivatives

A novel approach to nitro-substituted cyclopropanes and spiropentanes via oxidation of the corresponding amines with dimethyldioxirane is reported. The method is used successfully for the preparation of a series of nitrocyclopropanes as well as for the first synthesis of 1,4-dinitrospiro[2.2]pentane.     

Reaction of sodium N-benzylideneglycinate with dialkyl chlorophosphites in the presence of water

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On singularity and fine spectral structure of random continued fractions

We study properties of the distribution of a random variable of the continued fraction form where are independent and not necessarily identically distributed random variables. We prove the singularity of and study the fine spectral structure of such measures.     

Maps of several variables of finite total variation. II. E. Helly-type pointwise selection principles

Given a=(a₁,…,an), b=(b₁,…,bn)∈Rn with a<b componentwise and a map f from the rectangle into a metric semigroup M=(M,d,+), denote by the Hildebrandt-Leonov total variation of f on , which has been recently studied in [V.V. Chistyakov, Yu.V. Tretyachenko, Maps of several variables of finite total variation. I, J. Math. Anal. Appl. (2010), submitted for publication]. The following Helly-type pointwise selection principle is proved: If a sequence{fj}_j∈Nof maps frominto M is such that the closure in M of the set{fj(x)}_j∈Nis compact for eachandis finite, then there exists a subsequence of{fj}_j∈N, which converges pointwise onto a map f such that. A variant of this result is established concerning the weak pointwise convergence when values of maps lie in a reflexive Banach space (M,‖⋅‖) with separable dual M^∗.     

On positive commutators

Let A and B be positive operators on a Banach lattice such that the commutator C = AB − BA is also positive. We study the size of the spectrum of C.     

Hydrogen bonding in dimers of tritolyl and tritosylurea derivatives of triphenylmethanes

The crystal structure of the homodimer formed by the tritolylurea 3a proves the existence of a belt of six bifurcated hydrogen bonds between both NH and the O=C groups of the adjacent urea residues. For the tritosylurea 3b, four additional three-center hydrogen bonds, also involving the SO2 oxygen, are found in the crystalline state. Molecular dynamics simulations in a chloroform box confirm these patterns of the hydrogen bonds and the resulting elongation of the dimer 3b. 3b in comparison to 3a x 3a. The calculated complexation energies for the three dimeric combinations are nearly identical in agreement with the simultaneous formation of heterodimer 3a x 3b in a mixture of 3a and 3b.     

Synthesis and Pharmacological Evaluation of Novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole Derivatives as Promising Anxiolytic and Analgesic Agents

A number of novel 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole derivatives 2 were obtained by alkylation mainly in the 1H-tautomeric form of 2,3,4,5-tetrahydro[1,3]diazepino[1,2-a]benzimidazole or its 8,9-dimethyl-substituted analog 4-chlorobenzyl bromide, 4-chloroacetic acid fluoroanilide, and 4-tert-butylphenacyl bromide in neutral medium. Compounds 3 were cyclized and synthesized earlier with 11-phenacyl-substituted diazepino[1,2-a]benzimidazoles upon heating in conc. HBr. The chemical structures of the compounds were clarified by using the ¹H Nuclear Magnetic Resonance Spectroscopy (¹H-NMR) technique. Anxiolytic properties were evaluated using the elevated plus maze (EPM) and open field (OF) tests. The analgesic effect of compounds was estimated with the tail flick (TF) and hot plate (HP) methods. Besides, possible the influence of the test compounds on motor activities of the animals was examined by the Grid, Wire, and Rotarod tests. Compounds 2d and 3b were the most active due to their prominent analgesic and anxiolytic potentials, respectively. The results of the performed in silico analysis showed that the high anxiolytic activity of compound 3b is explained by the combination of a pronounced interaction mainly with the benzodiazepine site of the GABA_A receptor with a prominent interaction with both the specific and allosteric sites of the 5-HT_2A receptor.