Betulin-3,28-diphosphate (BDP) obtained by phosphorylation of betulin using POCl₃ has two main structural forms—BDP-1 and BDP-2—which differ in ethanol solubility, melting point, FTIR spectra, thermoanalytical characteristics and biological activity. Betulin-3,28-diphosphate and its sodium salt (Na-BDP) were characterized using ¹³C and ³¹P-NMR spectra, powder XRD experiments, as well as differential scanning calorimetry (DSC) and thermogravimetric analysis (TG) methods. The exo-effects at 193 ± 8 °C for ethanol soluble BDP-1 samples (−19.7 ± 0.2 kJ∙mol⁻¹) were about three times less than for ethanol insoluble BDP-2 samples f (−70.5 ± 0.7 kJ∙mol⁻¹). The DSC curves of Na-BDP-1 and Na-BDP-2 characterized the endo-effects having a maximum at 95–112 °C. Water-soluble Na-BDP-1 was obtained as needle-like crystals, unlike poorly crystalline Na-BDP-2, whereas BDP-1 and BDP-2 aged with time and were isolated as amorphous substances. In vitro experiments on rats showed that compared to the control, Na-BDP-1 increased catalase and SOD activity and improved energy metabolism more effectively than Na-BDP-2.

This study looked into the synthesis and study of Dextrane Sulfate–Doxorubicin Nanoparticles (DS–Dox NP) that are sensitive to amylase and show anticoagulant properties. The particles were obtained by the method of solvent replacement. They had a size of 305 ± 58 nm, with a mass ratio of DS:Dox = 3.3:1. On heating to 37 °C, the release of Dox from the particles was equal to 24.2% of the drug contained. In the presence of amylase, this ratio had increased to 42.1%. The study of the biological activity of the particles included an assessment of the cytotoxicity and the effect on hemostasis and antitumor activity. In a study of cytotoxicity on the L929 cell culture, it was found that the synthesized particles had less toxicity, compared to free doxorubicin. However, in the presence of amylase, their cytotoxicity was higher than the traditional forms of the drug. In a study of the effect of DS–Dox NP on hemostasis, it was found that the particles had a heparin-like anticoagulant effect. Antitumor activity was studied on the model of ascitic Zaidel hepatoma in rats. The frequency of complete cure in animals treated with the DS–Dox nanoparticles was higher, compared to animals receiving the traditional form of the drug.

Vinyl phenyl sulfone, methyl ( E)-3-(phenylsulfonyl)- and methyl ( E)-3-( p-tosyl)acrylates, ( E)-3-(phenylsulfonyl)- and ( E)-3-( p-tosyl)acrylonitriles react in ethyl ether at 20°C with...

Thermal van Alphen–Hüttel rearrangement of methyl 3,3-diphenyl-3-pyrazole-4-carboxylate, 3,3-diphenyl-3-pyrazole-4-carbonitrile, and methyl 5-methyl-3,3-diphenyl-3-pyrazole-4-carboxylate involves completely regioselective migration of one phenyl group from the 3-position to N with formation of aromatic 1-pyrazole system. Thermal rearrangement of methyl 3,3-diphenyl-3-pyrazole-5-carboxylate leads to the formation of methyl 4,5-diphenyl-1-pyrazole-3-carboxylate as a result of migration of the 3-phenyl group exclusively to the C atom and subsequent prototropic isomerization. Under analogous conditions, methyl 4-methyl-3,3-diphenyl-3-pyrazole-5-carboxylate, methyl 5-(methanesulfonyl)-3,3-diphenyl-3-pyrazole-4-carboxylate, methyl 5-(benzenesulfonyl)-3,3-diphenyl-3-pyrazole-4-carboxylate, and dimethyl 3,3-diphenyl-3-pyrazole-4,5-dicarboxylate have been regioselectively converted into the corresponding 4-pyrazoles. Thermolysis of 5-(4-methylbenzenesulfonyl)-3,3-diphenyl-3-pyrazole-4-carbonitrile gives rise to a mixture of 1- and 4-pyrazoles, the former considerably prevailing, whereas the corresponding 1-pyrazoles are formed as the only product from 5-(methanesulfonyl)- and 5-(benzenesulfonyl)-3,3-diphenyl-3-pyrazole-4-carbonitriles.

Tricyclo[4.1.0.02,7]heptane and 1-phenyltricyclo[4.1.0.02,7]heptane reacted with 2,3-bis(benzenesulfonyl)propene in boiling toluene (20–24 h) in the presence of benzoyl peroxide via trans-selective...