The synthesis of 1,4-diazacycl[3,2,2]azine

The diazaanalog of “cycl[3,2,2]azine”, “1,4-diazacycl[3,2,2]azine” (1,4,7b-triazacyclopent-[cd]indene) and its 2-methyl derivative were prepared. These compounds are subject to facile acid-catalyzed hydrolysis affording substituted imidazo[1,2-a]pyridines.     

Nucleophilic substitution in 5,6,7,8-tetrafluoro- and 6,7-difluoro-1,2,3,4-tetrahydro-9-alkenyl-1,4-methanonaphthalenes and related compounds. A search for homoallylic conjugation

The second-order rate constants for the nucleophilic replacement of fluorine by isopropoxide in 5,6,7,8-tetrafluoro- and 6,7,-difluoro-1,2,3,4-tetrahydro-9-alkenyl-1,4-methanonaphthalenes and related 9-alkyl systems have been measured. A factor of 6 - 7 separates the most reactive compounds [the 9- (4′-trifluoromethylbenzylidene) derivatives] from the least reactive compounds [the syn-9-isopropyl derivatives] in both the tetrafluoro- and difluoro-series. It is concluded for these small reactivity differences.     

Submanifolds of complex space forms admitting an almost contact metric compound structure

Summary Real hypersurfaces of an almost Hermitian manifold naturally admit an almost contact metric structure and the (f, g, u, v, w, , , )-structure is defined on submanifolds of codimension 3 of an almost Hermitian manifold. We study the so-called semi-invariant submanifolds of a complex space form with almost contact metric compound structure which is a general notion of (f, g, u, v, w, , , )-structure.Dedicated to professor Eulyong Pak on his 60th birthdayThis research was partially supported by Korean Science and Engineering Foundation Grant.     

Fabrication of hollow palladium spheres and their successful application to the recyclable heterogeneous catalyst for suzuki coupling reactions

Novel palladium hollow spheres were synthesized using silica spheres as a template, and they were successfully applied as recyclable heterogeneous catalysts for Suzuki cross coupling reactions.     

The reaction of 2-picoline N-Oxide with o-substituled benzoates and lsatoic anhydrides

The reaction of 2-picoline N-Oxide anion with o-substituted henzoates and isatoic anhydrides to give synthetically useful l-(2-methoxyphenyl)-2-(2-pyridinyl)ethanone N-oxides, I-(2-hydroxy-phenyJ)-2-(2-pyridinyl)ethanone N-oxides and I -(2-arninopheny])-2-(2-pyridinyl)ethanone N-oxides is described.     

The chemical behaviour of cobalt-stabilized carbenes having a trisubstituted silyl or germyl ligand. Stereospecific formation of benzoylsilanes from the reaction of organosilyl-cobalt tetracarbonyl derivatives with phenyllithium

We report the chemical behavior of cobalt-stabilized carbenes, R₃M(CO)₃CoC(OEt)R′, and their parent anions, R₃M(CO)₃CoC(O^?)R′, where M = Si or Ge. The anions where M = Si, R′ = Ph decompose thermally into the corresponding benzoylsilanes; when the silicon atom is chiral (R₃ = MePh-1-Np) optically active R₃SiCOPh is obtained with complete retention of configuration.     

Molecular characteristics of the inhibition of human neutrophil elastase by nonsteroidal antiinflammatory drugs

Nonsteroidal antiinflammatory drugs(NSAIDs) are known as clinically effective agents for treatment of inflammatory diseases. Inhibition of cyclooxygenase has been thought to be a major facet of the pharmacological mechanism of NSAIDs. However, it is difficult to ascribe the antiinflammatory effects of NSAIDs solely to the inhibition of prostaglandin synthesis. Human neutrophil elastase (HNElastase; HNE, EC 3.4.21.37) has been known as a causative factor in inflammatory diseases. To investigate the specific relationship between HNElastase inhibition and specificity of molecular structure of several NSAIDs, HNElastase was purified by Ultrogel AcA54 gel filtration, CM-Sephadex ion exchange, and HPLC (with TSK 250 column) chromatography. HNElastase was inhibited by aspirin and salicylate in a competitive manner and by naproxen, ketoprofen, phenylbutazone, and oxyphenbutazone in a partial competative manner, but not by ibuprofen and tolmetin. HNElastase-phenylbutazone-complex showed strong Raman shifts at 200, 440, 1124, 1194, 1384, 1506, and 1768 cm(-1). The Raman bands 1194, 1384, and 1768 cm(-1) may represent evidences of the conformational change at -N=N-phi radical, pyrazol ring, and -C=O radical of the elastase-drug complex, respectively. Phenylbutazone might be bound to HNElastase by ionic and hydrophobic interaction, and masked the active site. Inhibition of HNElastase could be another mechanism of action of NSAIDs besides cyclooxygenase inhibition in the treatment of inflammatory diseases. Different inhibition characteristics of HNE-lastase by NSAIDs such as aspirin, phenylbutazone-like drugs and ineffective drugs could be important points for drawing the criteria for appropriate drugs in clinical application.