A series of novel N-(3-substituted aryl/alkyl-4-oxo-1,3-thiazolidin-2-ylidene)-4-[5-(4-methylphenyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl]benzenesulfonamides 2a-e were synthesized by the addition of ethyl a-bromoacetate and anhydrous sodium acetate in dry ethanol to N-(substituted aryl/alkylcarbamothioyl)-4-[5-(4-methylphenyl)-3-(trifluoro-methyl)-1H-pyrazol-1-yl]benzene sulfonamides 1a-e, which...

Quinoline-2-carbohydrazide (3) was reacted with aryl or alkyl isothiocyanates to give the corresponding quinoline thiosemicarbazides (4a-e). Cyclization of the substituted thiosemicarbazides with sodium hydroxide led to the formation of 5-(quinolin-2-yl)2H-1, 2, 4-triazole-3(4H)-thiones (5a-e). Desulfurization of thiosemicarbazides by mercuric oxide gave 5-(quinolin-2-yl)-1, 3, 4-oxadiazol2-ami...

An efficient and convenient method was developed for the one-step synthesis of various substituted ethyl 2-(1H-indol-2-yl) acetates via a palladium-catalyzed regioselective cascade C-H activation reaction. Importantly, this practical approach can be carried out with readily accessible starting materials and exhibits excellent functional group compatibility. chemistry, methods for regioselective...

Abstract: 5,5 ′ -Methylenebis(4–phenyl-4H -1,2,4-triazole-3-thiol) (2) was synthesized starting from hydrazinecarbothioamide compound (1). Treatment of compound 2 with ethyl bromoacetate produced diethyl 5,5 ′ -{methylenebis[(4phenyl-4H -1,2,4-triazole-5,3-diyl)thio]}diacetate (3), which was converted to the corresponding diacetohydrazide derivative (4) by treatment with hydrazine hydrate. The ...

The homology of angiogenin and pancreatic RNase A provides a compelling reason to systematically compare the characteristics of the two proteins using the chemical modification approaches that proved essential to understanding the action of RNase. Reagents specific for histidine, lysine, and arginine markedly decrease the ribonucleolytic activity of angiogenin, much as has been observed for RNa...

The eyes of some crustaceans store substantial amounts of retinyl esters, with most of the retinol in the 11-cis configuration. Earlier work in this laboratory suggested that in lobster and crayfish the mechanism of isomerization of retinol to the 11-cis form involves the hydrolysis of all-trans retinyl esters. Although this is the same process as that occurring in the vertebrate eye, it is dif...

Described is the preparation of five sLex dimers and five sLex carboxylic acids by coupling chemoenzymatically synthesized amino-substituted sialyl Lewis x (sLex) derivative 4 to homobifunctional cross-linkers 20-24 of varying chain length. 20-24 were obtained by alkylating lowmolecular-weight oligoethylene glycols with tert-butyl bromoacetate and subsequent transformation of the di-tert-butyl ...

1-(2,4-Dichlorophenyl)-3-(4-fluorophenyl)propen-1-one (1) was prepared and reacted with an active methylene compound (ethyl cyanoacetate) in the presence of ammonium acetate to give the corresponding cyanopyridone 2. Compound 2 reacted with hydrazine hydrate, malononitrile, ethyl bromoacetate and phosphorous oxychloride to afford compounds 4 and 7-11, respectively. The 2-chloropyridine derivati...

A new series of heterocycles incorporating antipyrine moiety were synthesized via reactions of 4-aminoantipyrine 1 with carbon disulphide then alkylation and /or chloroacetic acid to produce dithiocarbamate and rhodanine 3, 4 and 9. Multi-component reaction (MCR) of 4-aminoantipyrine with carbon disulfide and DMAD afforded rhodanine 7. The interaction of 9 with diazonium salt, DMF-DMA, nitrous ...

In this study, theophylline (1) compounds were synthesized with addition of 2-bromoetha-nol, 2-bromoacetamide and methyl-2-bromoacetate to attain symmetric connections NHCs (2a–c). New complexes containing the N-heterocyclic carbene (NHC) ligands using azolium salts in dimethyl formamide (DMF). After NHC predecessor reacted Ag2O, Ag(I)-NHC following: 7,9-di-(2-hydroxyethyl)-8,9-dihydro-1,3-dime...