Solid-phase synthesis of 2,3-diphenylpropionic acid library as VLA-4 antagonists

2,3-Diphenylpropionic acid library for VLA-4 antagonist was synthesized on solid-phase. Comparison of the two synthetic routes via an orthogonal generation of two aromatic amino functional groups are discussed. From this work, several compounds were identified as potent VLA-4 antagonists.     

Cationic liposomes enhanced firefly bioluminescent assay of bacterial ATP in the presence of an ATP extractant.

Cationic liposomes composed of two components, diethylaminoethyl-carbamoyl cholesterol and phosphatidylcholine, were applied to an enhancer for a firefly bioluminescent (BL) assay of bacterial ATP in the presence of an ATP extractant. Trichloroacetic acid (TCA), which inhibits the activity of luciferase, was used as an ATP extractant. Cationic liposomes enhanced the BL intensity as long as luciferase was active. The detection limits for cell numbers of Escherichia coli extracts in the presence of cationic liposomes and in water alone were 199 and 897 colony forming units ml(-1), respectively. The sensitivity for bacterial ATP in the presence of cationic liposomes was improved by a factor of 2.5 times compared to that in the presence of diethylaminoethyl-dextran.     

Selective sulfonation of a secondary hydroxyl group of β-cyclodextrin

Tosylation of the secondary side of β-cyclodextrin, which has previously been incorrectly reported, can be achieved by tosyl transfer from 3-nitrophenyl toluenesulfonate to the C-2 hydroxyl of the cyclodextrin.     

Palladium(O)-catalyzed allylic alkylation and amination of allylic phosphates

Allyl diethyl phosphates (1) can be easily substituted with malonates and amines in the presence of palladium(O) catalyst. Synthetic utility of the reaction is demonstrated by the sequential amination-amination and alkylation-amination of (Z)-4-acetoxybut-2-enyl diethyl phosphate (1b) with high regio- and stereoselectivity.     

A statistical theory of nuclear neutrino capture

A statistical theory is proposed for the calculation of the total capture cross section of a neutrino by a nucleus. Close references are made to the statistical theory of β-decay and electron capture developed by Yamada and his collaborators. As a test of the theory, we calculate the total cross section for the capture of a solar neutrino by a ³⁷Cl nucleus.     

Thermal and photochemical reactions of a stable thiobenzaldehyde, 2,4,6-tri-t-butylthiobenzaldehyde

Thermal and photochemical reactions of the title compound gave benzothiolane $\text{2}$ in high yield; the reaction with free radicals also afforded $\text{2}$ along with some other products.     

Effects of carbon filler on sorption and diffusion of gases through rubbery materials

Effects of carbon filler on the sorption and diffusion of carbon dioxide in natural rubber and in styrene-butadiene rubber have been studied. Sorption isotherms conform to Henry's law in unfilled rubber and to Langmuir's law in carbon black. The isotherms in filled rubber exhibit a combination of the two sorption modes. The Henry's law solubility parameter k_D increases with carbon filler content; the Langmuir saturation constant C′_A initially is constant with filler level, but then decreases abruptly when carbon particles begin to aggregate. The diffusion coefficient decreases with increasing filler content, presumably owing to geometric effects and to polymer chain immobilization in the interfacial regions.