5-Fluorouracil derivatives. XX. Synthesis and antitumor activity of 5'-O-unsaturated acyl-5-fluorouridines

Various kinds of 5'-O-unsaturated acyl 5-fluorouridines were synthesized to obtain 5-fluorouridine derivatives with low toxicity and high antitumor activity. Antitumor activity of the compounds against L-1210 leukemia in mice was examined, and the 5'-O-4-pentenoyl derivative showed the highest antitumor activity.     

Sustainable domino Michael reaction catalyzed by a Brønsted base on silica gel: synthesis of bicyclo[2.2.2]octane-2,5-dione derivatives

Domino Michael reactions of oxophorone and its derivatives 4 with Michael partners 3 have been effected to give bicyclo[2.2.2]octane-2,5-dione derivatives 7 by a catalytic amount of a Brønsted base (NMAP-Li) generated from N-methylaminopropylated silica gel (NMAP) and n-BuLi. The NMAP pellets were efficiently reused up to six times in 86% average yield.     

Total synthesis of (+)-obtusenyne

The stereoselective total synthesis of (+)-obtusenyne is described. The oxonene skeleton possessing trans-orientated alkyl substituents at the α,α′-positions was stereoselectively constructed via cyclization of the corresponding hydroxy epoxide promoted by Eu(fod)₃.     

Diffraction and re-initiation of detonations behind a backward-facing step

Diffraction phenomena of gaseous detonation waves behind a backward-facing step in a tube are observed by using high-speed schlieren photography and soot-track records as well as by pressure measurements on the sidewall. Mixtures are stoichiometric oxyhydrogen and those diluted by argon at sub-atmospheric pressures. Three types of phenomena are observed, that is, continuous propagation of detonation, re-initiation after a temporal extinction of detonation and complete extinction of detonation. The continuous propagation means that the diffracted wave does not affect the main propagation although reflected shock waves from the bottom surface of the tube may affect it. The re-initiation occurs at a wall surface of the tube behind a reflected shock wave after the main detonation wave has been extinguished. Positions and conditions of the re-initiation are discussed. The complete extinction is defined as disappearance of detonation cells behind the step within a certain length of the tube. Cases exist where an ignition occurs after several reflections off the bottom and top surface of the tube.     

Elektronenspektren von 1,1-Diphenyl?thylen und Benzophenon

Ohne Zusammenfassung     

Measuring technique for static electricity using focused sound

A novel method is proposed for non-contact measurement of the distribution of electrostatic charge on a surface based on scanning the sample surface with a focused high frequency acoustic beam to excite movement of the sample surface. An electric field is induced by exciting a charged film-like object, and an electric field sensor measures it instead of an electrostatic field. The focused ultrasound waves are generated by controlling individually the phase of each 285 airborne ultrasound transducers.     

Total synthesis of valeriananoids A, B, and C via autocatalytic diastereoselective domino Michael reaction

Natural enantiomers of unique tricyclic sesquiterpenoids, valeriananoids A-C 1-3, have been synthesized starting from bicyclo[2.2.2]octane-2,5-dione derivative 11, which was obtained by diastereoselective catalytic domino Michael reaction of oxophorone 5 with 8-phenylmenthyl acrylate 10 by LDA or silica-gel-base (NMAP-Li). The tricyclic ring was closed selectively by intramolecular 6-endo-trig mode cyclization of the ketyl radical, which was generated from keto-allylether 25 by either lithium or sodium naphthalenide.     

Application of extraction chromatography to the separation of thorium and uranium dissolved in a solution of high salt concentration

Extraction chromatography with commercially available UTEVA resin (for uranium and tetravalent actinide) was applied for the separation of Th and U from control solutions prepared from a multi-element control solution and from sample solutions of solidified simulated waste. Thorium and U in control solutions with 1-5mol/dm(3) HNO(3) were extracted with UTEVA resin and recovered with a solution containing 0.1mol/dm(3) HNO(3) and 0.05mol/dm(3) oxalic acid to be separated from the other metallic elements. Extraction behavior of U in the sample solutions was similar to that in the control solutions, but extraction of Th was dependent on the concentration of HNO(3). Thorium was extracted from 5mol/dm(3) HNO(3) sample solutions but not from 1mol/dm(3) HNO(3) sample solutions. We conjecture that thorium fluoride formation interferes with extraction of Th. Addition of Al(NO(3))(3) and Fe(NO(3))(3), which have higher stability constant with fluoride ion than Th, does improve extractability of Th from 1mol/dm(3) HNO(3) sample solution.