A series of new C(2)-symmetric fluoren-9-ylidene malonate-derived bis(oxazoline) ligands were synthesized from fluoren-9-ylidene malonate and enantiomerically pure amino alcohols via a convenient route. Their asymmetric catalytic properties in the Friedel-Crafts reactions of indoles with arylidene malonates were evaluated, and the Cu(OTf)2 complex of a fluoren-9-ylidene malonate-derived bis(oxa...

Diclofenac sodium has been used for its anti-inflammatory actions for about 28 years, but since all the non-steroidal anti-inflammatory drugs (NSAIDs) suffer from the lethal gastro intestinal (GI) toxicities, diclofenac sodium is not an exception. The free –COOH group is thought to be responsible for the GI toxicity associated with all traditional NSAIDs. In the present research, the main motto...

A new route to 3-(4-arylmethylamino)butyl-5-arylidene-2-thioxo-1,3-thiazolidine-4-one 9 was developed in six steps from commercial 1,4-diaminobutane 1 as starting material. The key step of this multi-step synthesis involved a solution phase "one-pot two-steps" approach assisted by microwave dielectric from N-(arylmethyl)butane-1,4-diamine hydrochloride 6a-f (as source of the first point diversi...

Knoevenagel condensation between barbituric acid and aldehyde was investigated in the presence of sulfonic acid functionalized nanoporous silica (SBA-Pr-SO3H) and resulted in the formation of arylidene and bis-arylidene barbiturates. Excellent yields and short reaction times are related to the high efficiency of SBA-Pr-SO3H that the reactions take place easily in its nano-pores. SBA-Pr-SO3H as ...

A first synthesis of a new class of novel cytosine thioglycoside analogs from readily available starting materials has been described. The key step of this protocol is the formation of sodium pyrimidine-4-thiolate via condensation of N'-arylidene-2-cyanoacetohydrazides with sodium cyanocarbonimidodithioate salt, followed by coupling with halo sugars to give the corresponding cytosine thioglycos...

New series of 2,3-disubstituted quinazolin-4(3H)one were synthesized via the reaction of the readily obtainable 2-thioxo-3-phenyl-quinazolin-4(3H)one 1 with ethyl chloroacetate followed by hydrazinolysis to afford the hydrazide 3 which allowed to react with different electrophilic reagents such as carbon disulphide, phenyl isothiocyanate, β-diketones, anhydrides, acrylonitrile, ethyl cinnamate,...

The sequential sulfonylation/desulfination reactions of 5-benzylthiohydantoin with excess arylsulfonyl chlorides in the presence of triethylamine have been developed to afford a wide range of 5-arylidene thiohydantoin derivatives in moderate to excellent yields. A plausible sulfonylation/desulfination mechanism was proposed. The bioassay showed that these compounds exhibit certain fungicidal ac...

Complexes of arylidene salicyloyland benzoyl-hydrazones with the 3d metal ions, C r(III), M n(II), F e (III), C o (II), N i(II) and C u (II), have been prepared using 2:1 ligand to metal ion ratio. Characterization of the isolated solids was accomplished by IR and electronic spectra, elemental analysis, and molar conductivity measurements. It is concluded that the two Schiff bases function as n...

Novel 11-substituted 3,11-dihydro-2H-benzo[6,7]thiochromeno[2,3-d][1,3]-thiazole-2,5,10-triones 4a-i were synthesized in 75-90% yields via the hetero-Diels-Alder reaction of 5-arylidene-4-thioxo-2-thiazolidinones with 1,4-naphthoquinone. The synthesized compounds were evaluated for their antineoplastic and antimycobacterial activities. A moderate selectivity against melanoma cancer cells (GI50 ...

The first total synthesis of the dimeric alkaloid pigment scytonemin is described. The key transformations in its synthesis from 3-indole acetic acid are a Heck carbocyclization and a Suzuki-Miyaura cross-coupling, orchestrated in a stereospecific tandem fashion, followed by a biosynthetically inspired oxidative dimerization. The tandem sequence generates a tetracyclic (E)-3-(arylidene)-3,4-dih...