The enantiomerically pure N- and C-protected derivatives of planar-chiral (3-amino-1,2-dicarba-closo-dodecaboran-1-yl)acetic acid (>99% ee) have first been obtained in good yields via a combination of HPLC separation and synthetic procedures. Assignment of absolute configuration of the carborane...
The kinetics of the hydrodesulfurization (HDS) of dibenzothiophene (DBT), 4,6-dimethyldibenzothiophene (4,6-DMDBT), and their hydrogenated intermediates over bulk tungsten phosphide (WP) was studied. WP possessed high hydrogenation/dehydrogenation activity but was highly sensitive to piperidine ...
Various pyridopyridazinone derivatives were designed as Poly(ADP-ribose) polymerase-1 (PARP-1) inhibitors. The pyridopyridazinone scaffold was used as an isostere of the phthalazine nucleus of the lead compound Olaparib in addition to some modifications in the tail part of the molecule. Prelimin...
The rates of acid cleavage of (pentafluorophenyl)trimethyl-stannane and -silane have been measured. For the first compound the rate is markedly larger than would be expected for additivity of the deactivating effects of the five fluorine atoms separately. For the second, the rate is not signific...
Reactions of Me3SiC6F5 and MF (M = Cs, [NMe4]) in molar ratios varying from 1:1 to 2:1 in a temperature range between −70 °C and ambient proceed more or less selectively to form 1-H-perfluoro-4,4′-polyphenyls, 1-H(C6F4)nF, independent of the solvent used (DME, THF). The silicates expected, M[M...
Hydrogen-bonding receptors for carboxylic acids have been prepared based on a cis tetrahydrobenzoxanthene skeleton. X-ray diffraction study of one of these compounds revealed that the cleft is suitable for establishing strong linear hydrogen bonds with the oxygen of a water molecule. Complexes t...
Saccharomyces cerevisiae, strain DBM 2115, was successfully employed in the reduction of the separated Z- and E-isomers of ethyl 4-[(2-oxocyclohexyl)methyl]phenoxy-3-methyl-2-butenoates 1 and 2, in order to prepare the (1S,2S)- and (1R,2S)-enantiomers of the corresponding ethyl 4-[(2-hydroxycycl...
Synthetic applications of ethyl 3-bromodifluoromethyl-3-benzyloxy-acrylate as a versatile and multifunctionalized gem-difluorination building block to introduce difluoromethene subunit into some new hydroxy esters have been investigated. It was found that its zinc mediated reaction with a variet...
The solvatochromic behavior of novel carbazole containing dyes obtained by the condensation of 9-ethyl-9H-carbazole-3-carboxaldehyde and 9-ethyl-9H-carbazole-3,6-dicarboxaldehyde with (1-phenylethylidene) propanedinitrile and ethyl-2-cyano-3-phenyl-2-butenoate are described. The dyes were charac...
The electrochemical oxidation of 3-methyldiphenylamine, 3-MeDPA, and 3-methoxydiphenylamine, 3-MeODPA, in lithium perchlorate CH3CN solutions produced either thin, uniform polymeric films on ITO electrodes or high quality, free-standing polymeric films with good electrochemical response. Thin po...
In this study, the structural and spectroscopic investigations of 3-methyldiphenylamine were reported. The molecular geometry was optimized from Density Functional Theory (B3LYP method) using 6-31+G(d,p) basis set on the ground state and the infrared wavenumbers and intensities were predicted by...
S,S-Dimethyl-N-(2,4-dinitrophenyl)sulfilimine(4a) has been prepared in good yield by use of DMSO, 2,4-dinitroaniline and phosphorus pentoxide in DMF and the role of DMF in this System is discussed. The method has been applied successfully to the syntheses of several sulfilimines. The reactions o...
Palladium-catalysed reactions of aryl iodides/vinyl triflates with 2,2,2-trifluoro-N-(2-(4-[2,2,2-trifluoro-acetylamino)-phenyl]-buta-1,3-diynyl)-phenyl)-acetamide provide a straightforward entry into 3,3′-disubstituted-2,2′-biindolyls. Subsequent application of the procedure to homochiral ary...
The crystal and molecular structures of methyl (N-benzoylaminooxy)acetate (MBAOA) have been determined by X-ray diffraction at room temperature. In the crystal the amide CO of one molecule is hydrogen-bonded to the amide NH of an adjacent molecule (O1 ⋯ N1′ = 2.850(2) Å, O1 ⋯ H6′N1′ = 15...
The synthesis of monomer, dimer, tricyclohexyl- and triphenyl-tin(IV) complexes with phthalimido-4-methyl pentanoic acid (PMPA) are described and characterized by FT IR, CHN analyzer, 1H, 13C 119Sn NMR and 119mSn Mössbauer spectroscopic techniques. In vitro ED50, anti-tumor (phytotoxic), anti-ye...
N-Hydroxymethylation and N-acyloxymethylation of weakly NH-acidic compounds such as carboxamides, carbamates and ureas are not useful approaches to obtain prodrug forms of such agents because of the too high stability of the N-hydroxymethyl derivatives at physiological pH and temperature. In an ...
Three new esters of aspirin were synthesized and evaluated in vitro as potential prodrug forms of aspirin with the aim of depressing the gastrotoxicity of the drug by temporarily masking the carboxylic acid function. The esters, derived from N-(hydroxymethyl)acetamide, N-(hydroxymethyl)benzamide...
4-Methylumbelliferyl esters of amino acid derivatives have been synthesized using the carbodiimide, disulphite and carbonate methods. Of these, the first was shown capable of preparing 2-naphthyl and 4-methylumbelliferyl esters of benzoylglycine, benzyloxycarbonyl glycine and benzyloxycarbonyl-c...
The triorganotin(IV) derivatives of N-benzoylglycine (HAA); R3SnAA and N-benzoylglycylglycine (HDP), R3SnDP (R = methyl, n-propyl, n-butyl, phenyl, cyclohexyl, respectively) have been prepared from the triorganotin(IV) chlorides R3SnCl and the appropriate sodium salts of the N-benzoylamino acids...
(Pivaloyloxy)methyl 6,6-dihalo-, 6α-monosubstituted- and 6α-halo 1,1-dioxide penicillanates, N-benzoylglycine methyl ester and several selected esters are efficiently hydrolyzed with bis(tributyltin) oxide (nBu3Sn)2O with yields from 43 to 100%.
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