A new series of pyrazoline derivatives 1b-12b was designed, synthesized and evaluated for antiproliferative activity against three cancer cell lines (HepG-2, Hela and A549). Additionally, NIH/3T3 cell cytotoxicity were tested and the structure activity relationships (SARs) were also determined. Among these new derivatives, the compounds 3-(4-fluorophenyl)-5-(3,4,5-trimethoxythiophenyl)-4,5-dihy...

The solvent-free reactions of β-enamino carbonyl compounds with 1-(pyridin-2-yl)-enones in the presence of manganese(iii) acetate dihydrate unexpectedly afforded 2-acyl-3-aryl-6,7-dihydro-4(5H)-benzofuran derivatives under mechanical milling conditions.

Upon Brønsted base organocatalysis, ketone-derived alkylidene Meldrum's acids proved to be competent vinylogous platforms able undergo a formal (4+2) cycloaddition reaction with dihydro-2,3-furandione, providing an unprecedented route 3,6-dihydropyran-2-ones as spiro[4.5]decane derivatives up 98 % ee thanks the commercially available Takemoto catalyst. Preliminary investigation showed that this...

A simple and efficient method has been developed for the synthesis of 4,5-dihydro-2-mercapto-4-oxo-6-substituted arylpyrimidine derivatives (2a-e) and their fused rings (3b, 4b, 5b & 6b) and also 1,4-dihydro-2-mercaptopyrimidine derivatives (7a-e) & (9a-e) using triethylamine as a catalyst. The structure of the newly synthesized compounds was confirmed on the basis of their spectral data and el...

The reaction of 2-methylene-1,3-dicarbonyl compounds (1) with ethyl diazoacetate gave 4,5-dihydro-1H-pyrazole derivatives (2), which were stable for several months at room temperature in good yields.

an efficient synthesis of trialkyl (e)-3-(3-oxo-2-3,4-dihydro-2-(1h)-quinoxalinylidene)-prop-1-ene-1,2,3-tricarboxylate derivatives via a simple three-component reaction between benzene-1,2-diamines with dialkyl acetylenedicarboxylates in the presence of k2co3-peg catalytic system at 100 oc was reported. the desired products were obtained in excellent yields (88-92%). various benzene-1,2-diamin...

Treatment of dialkylbenzylsilane (1) with trityl tetrakis(pentafluorophenyl)borate (TPFPB) in the presence of terminal or internal alkynes (3) and 2,6-di-tert-butyl-4-methylpyridine gave the corresponding 1,2-dihydro-2-silanaphthalene derivatives (4) in 34-82% yields.

Novel dihydro-1,3-oxazinoporphyrins and naphtho[e]bis(dihydro-1,3-oxazinoporphyrin) derivatives, in which the porphyrin macrocycle is covalently linked to the dihydro-1,3-oxazine ring system were successfully synthesized from 5-(4-aminophenyl)-10,15,20-triphenylporphyrin in good yields. The structures of the target products were established on the basis of spectral data and elemental analyses.

Reaction of thionyl chloride with 7-chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4- oxoquinoline-3-carboxylic acid 1 gave acid chloride 2. Compound 2 was reacted with glycine and D-glutamic acid to afford 2-(7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4- dihydroquinoline-3-carbonyl) aminopantandioicacid 3a and 2-(7-chloro-1-cyclopropyl-6- fluoro -4- oxo-1,4-dihydroquinoline-3-carbonyl)aminoacetica...