for its high cytotoxicity against several cancer cell lines due to its intercalating properties and its ability to inhibit DNA religation by topoisomerase II. A number of angular analogs have been prepared in order to obtain more active compounds. For example, one of the most promising products appeared to be intoplicine 2, synthesised firstly by Nguyen et al., which acts both as an intercalati...

The first example of the use of an N-heterocyclic carbene (NHC) as an organocatalyst for the activation of isocyanides was demonstrated. On the basis of previous reports on the interaction between NHCs and isocyanides, we developed a catalytic cycle involving transient imidoyl intermediate. The reaction of ketones with isocyanides produced the corresponding enaminones with high efficiency. Cont...

Present work employs the QSAR formalism to predict the ED(50) anticonvulsant activity of ringed-enaminones, in order to apply these relationships for the prediction of unknown open-chain compounds containing the same types of functional groups in their molecular structure. Two different modeling approaches are applied with the purpose of comparing the consistency of our results: (a) the search ...

* e-mail: [email protected] Present address: Instituto de Química, Universidade Federal da Bahia, Campus de Ondina, 40170-290 Salvador BA, Brazil. # Dedicated to Professor Albert James Kascheres, a great mentor and pioneer in ciclopropenone chemistry in Brazil, on the occasion of his 60th birthday. Reaction of Acyclic Enaminones with Methoxymethylene Meldrum’s Acid. Synthetic and Structural Impl...

Reactions of aldehydes, 1,3-indanedione and enaminones were successfully carried out using p-toluene sulfonic acid (p-TsOH) as a catalyst and high-temperature water as a solvent under microwave irradiation. This method provided several advantages such as rapid reaction times, high yields, and a simple workup procedure. In addition, a possible mechanism to account for the reaction was proposed.

An efficient one-pot, three-component method for the preparation of indeno[1,2-b]quinoline-9,11(6H,10H)-dione, acridine-1,8(2H,5H)-dione and various multi-substituted quinoline-3-carbonitrile derivatives has been developed through the Michael addition to enaminones, which was achieved by both microwave irradiation and conventional heating.

A C–N bond formation reaction under benign conditions for the amination of allenic ketones to access enaminones is reported. This atom economical, green, highly regioselective and works well with many structurally crucial amines.

The asymmetric synthesis of tetrahydropyridin-2-ols from enals and enaminones is described. The organocatalytic domino reaction involves a Michael addition-hemiaminalization sequence using the Jørgensen-Hayashi catalyst. Dehydration or oxidation leads to the corresponding 1,4-dihydro-pyridines or 3,4-dihydropyridin-2-ones in a one-pot fashion.

A peptide that functions only in the presence of a protein has been developed using reaction-based selection from peptide phage libraries. The peptide was not functional in the absence of the protein, but formed enaminones with 1,3-diketone derivatives when bound to the protein.