Some nucleophilic substitution reactions of s-triazolo[1,5-c]pyrimidines

Nucleophilic substitution of 5-methylthio- and 5-cyanomethylthio-7-amino-s-triazolo[1,5-c]pyrimidines has been carried out using sodium hydroxide, ammonia, hydrazine hydrate, and four amines. The cyanomethyl group is particularly reactive under these conditions and 5-cyanomethylthiotriazolopyrimidine can be used to functionalize this heterocycle.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 3, pp. 382–385, March, 1992.     

Keratinized epithelial transport of beta-blocking agents. I. Relationship between physicochemical properties of drugs and the flux across rat skin and hamster cheek pouch.

The maximum fluxes (Jmax) of beta-blockers through keratinized membranes were determined in vitro and compared with their physiochemical parameters such as lipophilicity (log k'0) and melting point (mp). Rat abdominal skin and hamster cheek pouch mucosa were used as the model membranes. Propranolol, metoprolol, timolol, pindolol, nadolol and agenolol were used as beta-blockers with a variety of physicochemical characters. Linear relations of Jmax with either log k'0 or mp were observed both in intact rat skin and in intact hamster cheek pouch, suggesting that the lipophilicity and thermodynamic activity of a drug in the crystal state primarily affect the drug's permeation through these membranes. However, the slope, dJmax/d(log k'0), for cheek pouch mucosa was greater than that for rat skin, corresponding to the lack of appendigeal shunt pathways in cheek pouch. Penetration studies using the delipidized membranes and the isolated stratum corneum sheet of hamster cheek pouch mucosa clarified that the primary rate-limiting barrier function might exist in the lipid layer of the stratum corneum. Jmax values for the tape-stripped and delipidized skins correlated with both the solubilities of drugs in the vehicle and with the mp, suggesting the polar porous characteristics of both model membranes. However, a theoretical approach confirmed that the contribution of an intracellular or aqueous pore route in the intact membrane to the permeation of drugs with positive lipophilic indexes is negligible.     

Measurements of total and positronium-formation cross sections for the scattering of positrons by alkali atoms

We present a review of our recent measurements of total cross sections (Q _T's) for the scattering of positrons by Na, K, and Rb, and positronium-formation cross sections (Q _Ps's) for Na and K. For our total cross section measurements, a beam transmission technique has been used. For ourQ _Ps measurements, our approach involves setting upper and lower limits onQ _Ps using a combination of (1) measuring the transmission of the positron beam with the angular discrimination of the apparatus made as poor as possible, and (2) measuring the 511 keV annihilation gamma rays in coincidence produced by the decay of para-Ps formed in the scattering cell. Comparison with theoretical calculations shows that our measuredQ _T's andQ _Ps's for Na and K agree reasonably well with a close coupling approximation (CCA) calculation which takes into account the formation of Ps in then=1 andn=2 states. In the 3–10 eV energy range, this calculation predicts a peak in theQ _T's andQ _Ps's for K which also appears in our measurements. The absence of such a peak in our measuredQ _T's andQ _Ps's (preliminary) for Na in this energy range is also consistent with the same theory. Comparisons with five-state CCA calculations ofQ _T which do not take Ps-formation into account also show good agreement with our positron-Na, K, and RbQ _T measurements for energies above 20 eV, but show dramatic departures from our measurements below 10 eV for K and Rb.     

Muon spin resonance and repolarization in amorphous silicon monoxide (a-SiO)

Studies of the muonium fractions in the amorphous oxide a-SiO have been carried out by RF resonance at TRIUMF, Canada and LF repolarization techniques at RAL, U.K. The resonance measurements confirm the presence of the interstitial Mu centre in this intermediate oxide of silicon. Analysis of the data gathered at RAL, using a recently-developed fitting technique, reveals that the Mu^* state is present here as well, but with lower relative fractions than in a-Si. However, as in the latter material, but in contrast to c-Si, this bond-centre species appears to be stable up to room temperature.     

Specular reflectance of cold-rolled aluminum surfaces

The specular reflectance of cold-rolled aluminum surface is studied using a fiber optic system. An approximation for the determination of surface roughness is presented.     

Average and local magnetic moments on Fe atoms in microcrystalline and amorphous Fe100−xPx alloys

We have measured the concentration dependence of the average magnetic moment per Fe atom _Fe(x) in microcrystalline and amorphous Fe-P alloys obtained over a wide concentration range using electrochemical deposition. The model of local magnetic moments has been used to described _Fe(x). On the basis of this model the effects of phosphorus on the value _Fe are explained in terms of the parameters of the local environment of the Fe atom.     

Europium-151 Mössbauer spectroscopic and XANES investigation of europium-exchanged Y-zeolite

Eu³⁺ in ca. 10 wt% europium-exchanged Y-zeolite is partially reduced by treatment in hydrogen at 600°C to Eu²⁺. The reduction of Eu³⁺ is more readily achieved in Y-zeolite than in europium(III) oxide. The discrepancy in the extent of reduction as revealed by¹⁵¹Eu Mössbauer spectroscopy and near edge X-ray absorption fine structure (XANES) is associated with any difference in the recoil free fractions of Eu²⁺ and Eu³⁺ which may exist at 298 K and the enhanced sensitivity of the XANES to changes in the europium oxidation state.