A novel approach based on combinations of various water compatible Lewis acids and L-proline cocatalysts has been evaluated for the direct asymmetric aldol reaction. From this screening zinc (II) chloride salts lead to the highest stereoselectivities. Optimized catalytic conditions (Catalytic system : L-proline : 20 (percent) / ZnCl2 : 10 (percent) - Solvent mixture : DMSO/H2O – 8 : 2) give anti aldol product with improved enantioselectivity (>99 (percent) e.e.) compared to a moderately stereoselective procedure based on proline activation only.

It was found that tetraethylammonium hydroxide reacts with N-hydroxyphthalimide as a nucleophile rather than a base to afford tetraethylammonium 2-(hydroxycarbamoyl)benzoate (TEAHCB). The TEAHCB was found to be able to efficiently catalyze the cyanosilylation of a wide range of carbonyl compounds as a bifunctional organocatalyst at very low catalyst loading (0.2 mol(percent)).

porphyrins were prepared inside the large pores of the zeolite NaY by a process of sequential introduction of components followed by assembly inside the void space of the zeolite. The appropriate process chosen for the porphyrin synthesis was using the propionic acid solvent for reaction between pyrrole and benzaldehyde and this solvent was not destructive for zeolite. The resulting materials were purified by Soxhlet extractor. The zeolite-included porphyrins were identified for studies using UV-Vis and FTIR Spectroscopy and SEM techniques.

We describe herein a novel synthetical application of shikimic acid, which consist of its transformation into (3R,4S,5R,7S)-7-(hydroxymethyl)azepane-3,4,5-triol.

A one- pot three-component reaction of 2-aminobenzothiazole, 2-naphthol, and aldehydes has efficiently been carried out in the presence of Wells-Dawson heteropolyacid (H6P2W18O62 _ 24H2O) in water at 60 °C to form the corresponding 2'-aminobenzothiazolomethylnaphthols in high yields.

A new proton sponge 1,8-bis(tetramethylguanidino)naphthalene (TMGN) was utilized for the alkylation of benzoic acid by iodomethane in a continuous flow microsystem. Using this set-up, kinetics of the reaction was determined in different mixing strategies and the Hammett reaction constant was measured. Good performance and efficiency of this procedure were confirmed through several preparative studies.

Evaluation of a new proton sponge, bis-1,1,8,8-(tetramethylguanidino)naphtalene (TMGN), in substituted phenols O-alkylation by methyl iodide in DMF has been studied. Kinetic measurements were performed in N,N-dimethylformamide-d7 and followed by 1H NMR using stoichiometric amounts of reagents. Plot of the results shows that the reaction follows an almost perfect second order rate law. However the Hammett plots for substituted phenols are not linear but bell shaped. In order to separate the deprotonation and alkylation contribution to the kinetics, deprotonation of phenols by TMGN has been investigated by quantitative 13C NMR. By combining these data a linear Hammett plot with a negative slope was obtained for the alkylation step and substituted phenol acidity constants in DMF, not accessible by NMR measurements, were determined which are in agreement with literature data.

A combinatorial library of alpha ketoamines was generated by the Ugi four component reaction on tertiary carboxylic acid.

Polymorphism of active pharmaceutical ingredients (APIs) gets increasing attention as an important physico-chemical parameter influencing bioavailability and stability of API and pharmaceuticals. Co-crystals of API with common pharmaceutical excipients become very important as a tool to tune up solubility and absorption. Bisphosphonates (e.g. alendronate, risedronate, ibandronate) are widely used in clinical practice. They are indicated for the treatment and prevention of osteoporosis. They are powerful inhibitors of bone resorption, but their gastrointestinal adsorption is only about 1(percent) due to their high hydrophilicity. Some experiments were designed to prepare co-crystals of ibandronate. In the present study various mixtures of ibandronate and excipients were prepared. All the prepared mixtures (solid compounds) and/or new entities were analyzed by means of FT-NIR spectroscopy. The absorption of potential new co-crystals was investigated by means of the PAMPA experiments.

5-BromoVerongamine has been successfully synthesized in 2 steps in good yield from readily available starting materials. Structural elucidation has been confirmed through direct comparison with spectroscopic data of isolated natural product. 5-BromoVerongamine has been shown to have moderate bacteriacidal activity against MRSA.