(E)-3-(2-Methyl-1H-indol-3-yl)-1-(4-methylphenyl)propenone has been prepared, and its crystal structure (C19H17NO, Mr = 275.34) has been determined by single-crystal X-ray diffraction analysis. The title compound crystallized in the triclinic system with space group P1 and unit cell parameters: a = 9.4014 (5) ?, b = 9.8347 (4) ?, c = 10.0318 (5) ?, ? = 62.821 (3)°, B = 85.539 (3)°, ? = 65.262 (3)° and Z = 2. The final reliability index is 0.053 for the 2807 observed reflections. The title compound is linked through N–H···O hydrogen bonds.
The immobilized NaHSO4·H2O on activated charcoal was used as a highly efficient promoter system for facile N-formylation of amines with ethyl formate. All reactions were carried out in refluxing ethyl formate (54 ?C) under mild conditions within 10-100 min to afford the product formamides in high to excellent yields (80-94%).
The E-1,3-diaminoethenyl functional group is a potentially useful synthon. A number of examples of E-1,3-diaminoethenyl functional groups were prepared in good yield starting from an E-enol tosylate of a serine based diketopiperazine and 1°- or 2° amine nucleophiles. The reaction proceeds via a stereoselective nucleophilic substitution pathway.
A series of new Schiff bases of 4-(methylthio)benzaldehyde derivatives 3(a-i) were synthesized by the reaction of 4-(methylthio)benzaldehyde with various amines 2(a-i). Newly synthesized compounds were characterized by elemental analyses, UV-visible, FT-IR, Mass and 1H NMR spectral studies. All compounds were evaluated for their in vitro antibacterial activity against clinically isolated strains i.e., E. Coli, P. Fluorescence, M. Luteus and B. Subtilis. These compounds were screened for their antioxidant activity by 2,2-diphenyl-1-picryl-hydrazyl (DPPH•) and ferrous ion chelating assay (Fe2+) methods. The cytotoxicity assay was performed by tryphan blue dye exclusion method. Compounds 3g, 3h and 3i exhibited good antibacterial activity when compared with other compounds in the series against tested pathogenic bacterial strains. All the compounds showed antioxidant activity, where compound 3b was the best radical scavenger and Fe2+ ion scavenger. These findings showed that the Schiff bases of 4-(methylthio)benzaldehyde derivatives possess antioxidant activity with different mechanism of actions towards the different free radicals tested. Among these derivatives, 3b and 3h had the strongest activity against human peripheral lymphocytes.
In our present investigation a new series of nucleoside derivatives (2-13) were synthesized from uridine (1) via only two step reactions by direct acylation method. Firstly, uridine (1) was treated with 4-t-butylbenzoyl chloride in pyridine at -5?C and afforded the 5´-O-(4-t-butylbenzoyl)uridine derivative (2) in an excellent yield. In order to obtain newer products, the 5´-O-uridine derivative was further transformed to a series of 2´,3´-di-O-acyl derivatives (2-13) containing a wide variety of functionalities in a single molecular framework. The yields of the compounds were more than 80%. The synthesized titled compounds were characterized by their physical properties, FTIR (Fourier transform infrared spectroscopy), 1H-NMR (Nuclear magnetic resonance) spectroscopy and elemental analysis.