Novel derivatives of 5-(substituted)benzylidene-3-(4-substituted)phenylsulfonylimidazolidine-2,4-diones (3a-r), 1-(4-substituted)phenylsulfonyl-3-(4-substituted)phenylpyrimidine-2,4,6-(1H,3H,5H)-triones (6a-l), and 3-(4-substituted)phenyl-1-(4-substituted)phenylsulfonylquinazoline-2,4(1H,3H)- diones (8a-l) have been synthesized and tested for their antitumor activity against 60 tumor cell lines...

      Reaction of 5-phenyl tetrazole with ethyl chloroacetate to form ethyl (5-phenyl-1H-tetrazol-1-yl) acetate (1). Compound 1 react with hydrazine hydrate in ethanol yield 2-(5-phenyl-1H-tetrazol-1-yl) acetohydrazide (2). The condensation of (2) with various aldehydes yield the corresponding substituted N'-[-arylidene]-2-(5-phenyl-1H-tetrazol-1-yl) acetohydrazide (3a- j). Th...

Reactions of N,N;-disubstituted hydrazinecarbothioamides 8a-c and substituted thioureidoethylthioureas 9a-c with 2,3,5,6-tetrachloro-1,4-benzoquinone (chloranil, 10a) and 2,3,5,6-tetrabromo-1,4-benzoquinone (bromanil, 10b) to form N,N;-disubstituted [1,3,4]thiadiazole-2,5-diamines 11a-c, 6,7-dichloro-3-substituted amino-1H-benzo[1,3,4]- thiadiazine-5,8-diones 12a-c, 2,3,7,8-tetrahalothianthrene...

The synthesis of 3,4-dihydro-1,2-oxazepin-5(2H)-ones and 2,3-dihydropyridin-4(1H)-ones from β-substituted β-hydroxyaminoaldehydes is reported. The β-hydroxyaminoaldehydes were prepared by enantioselective organocatalytic 1,4-addition of N-tert-butyl (tert-butyldimethylsilyl)oxycarbamate to α,β-unsaturated aldehydes (MacMillan protocol). Alkyne addition to the aldehydes followed by alcohol oxida...

calix(6)arene hydroxamic acids (iii) are synthesised for the first time by reactingcalix(6)arene acid chloride(ii) with substituted hydroxylamines at low temperature in the presence ofsodium bicarbonate. the p-carboxycalix(6)arene(i) is obtained by an acid catalysed condensationreaction of p-hydroxybenzoic acid and formaldehyde. these calixarenes are characterised by meltingpoint, uv, ir, 1h nm...

A series of methyl 6-Chloro-2-Substitued-1-[2-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]1H-benzoimidazol-5-ylamine were successfully synthesized. Benzimidazoles were prepared by condensation of 4-chloro-o-phenylenediamine with substituted aryl, aldehyde condensation with biphenyl tetrazole group and reduction stannous chloride dihydrate. An insertion-cyclization strategy was involved during synthe...

Alkylation of quinolin-2(1H)-one (1) and its C(6) and C(7) substituted dervatives (OMe, OBn, and Cl) with 2-bromoacetophenone or chloroacetone under basic condition (K2CO3 in DMF) gave a mixture of N1and O2alkylated products with the former one as a major product. However, alkylation of 8-methoxy-, 8-benzyloxy-, and 8-chloroquinolin-2(1H)-ones under the same reaction conditions gave exclusively...

An efficient synthesis of 1,3-diaryl-4-halo-1H-pyrazoles was achieved. The synthesis involves the [3 + 2] dipolar cycloaddition of 3-arylsydnones and 2-aryl-1,1-dihalo-1-alkenes. The process proceeds smoothly in moderate to excellent yields. 1,3-Diaryl-4-halo-1H-pyrazoles are found to be important intermediates that can easily be converted into 1,2,5-triaryl-substituted pyrazoles via Pd-catalyz...

A new series of 5-substituted-3-methylsulfanyl-1-(2,4-dinitro phenyl)-1H-pyrazole-4-carboxylic acid ethyl esters were synthesized by reacting the amino group of 5-amino-3-methylsulfanyl-1-(2,4-dinitro phenyl)-1H-pyrazole-4carboxylic acid ethyl ester with acid anhydrides, acid chlorides and phenyl dithiocarbamates. The title compounds were investigated for analgesic, anti-inflammatory and ulcero...

Substituted 3,4-dihydro-1,8-naphthyridin-2(1H)-ones have been synthesized with the inverse electron-demand Diels-Alder reaction from 1,2,4-triazines bearing an acylamino group with a terminal alkyne side chain. Alkynes were first subjected to the Sonogashira cross-coupling reaction with aryl halides, the product of which then underwent an intramolecular inverse electron-demand Diels-Alder react...