Band 20, Heft 1

New 2-(1,2,3-triazol-1-yl)pyrimidines were synthesized in good yields by the three-component reaction of pyrimidin-2-yl sulfonates, sodium azide and active methylene ketones in the presence of K 2 CO 3 at room temperature. This procedure eliminates the need to handle organic azides in the synthesis of analogous compounds.

Nucleophilic displacement of chlorides in 3,3′-dichloro-5,5′-bi-1,2,4-triazine with benzenethiolate or 2-pyridinethiolate anion afforded the corresponding symmetrical disulfide of 5,5′-bi-1,2,4-triazine in high yields. These products were transformed into 6,6′-bis(phenylthio)-2,2′-bipyridines and 6,6′-bis(2-pyridylthio)-2,2′-bipyridines by using Diels-Alder reactions. All compounds were fully characterized by spectroscopic methods and the X-ray diffraction analysis.

An efficient synthetic approach to the synthesis of the 5-pyrimidinecarbaldehyde 2 , which is the key intermediate of rosuvastatin, involves the aerobic oxidation of the 5-pyrimidinemethanol 1 in the presence of Co(NO 3 ) 2 , dimethylglyoxime (DmgH 2 ), and 2,2,6,6-tetramethylpiperidine-1-oxyl (TEMPO) under mild reaction conditions. The method does not require the use of hazardous or expensive chemicals and is suitable for scale-up.

A series of multifunctional hindered amine light stabilizers (HALSs) for monomers were designed and synthesized from cyanuric chloride, allylamine, 2,2,6,6-tetramethylpiperidine-4-ol or 1,2,2,6,6-pentamethylpiperidine-4-ol, and 2-(2-hydroxyphenyl)-1,2,3-benzotriazole derivatives through nucleophilic substitution. The new stabilizers were confirmed by 1 H NMR, 13 C NMR, FT-IR, ESI-HRMS and elemental analysis. The synthesized compounds 5a–f were evaluated for their antioxidant and anti-aging properties. The results indicate that the new HALSs can considerably improve polymer photostability.

Treatment of N , N -dimethyl- N ′-(2-pyridyl)formamidine with methyl vinyl ketone under microwave irradiation yields N -formyl- N -(3-oxobutyl)-2-pyridylamine without decomposition or polymerization of methyl vinyl ketone. The result is an alternative non-oxidative approach to the preparation of N -formyl-substituted aminoketones.

A series of 2-thienyl substituted derivatives of thiazoles, oxazoles and spiro(indole-azole) were synthesized. The structures of the synthesized compounds were confirmed by IR, NMR and mass spectral data.

2-Amino-5-mercapto-1,3,4-thiadiazole (AMT) was used to synthesize 24 new compounds. The structures were confirmed by 1 H NMR and 13 C NMR.

A green procedure was developed for the condensation of isatin and N -substituted isatins with 1,2-diaminobenzene by using reusable bentonite clay in EtOH/H 2 O solvent system, under microwave irradiation. This eco-friendly synthesis is characterized by high yields and short reaction times. The catalyst is easily recycled.

Synthesis, characterization and investigation of antimicrobial activities of seven new 6-(1,3-thiazol-4-yl)-1,3-benzoxazol-2(3 H )-ones are presented. Their structures were determined using 1 H NMR, 13 C NMR and elemental analyses. The compounds possess some biological activity against Gram-positive bacteria, especially against Micrococcus luteus belonging to opportunistic pathogens, with an MIC of 31.25 μg/mL.

A novel and efficient synthesis of (+)-preussin ( 7 ) starting from N -butoxycarbonyl-L-phenylalaninal ( 1 ) is described. This natural product was synthesized under mild conditions and with good overall yield.

A single crystal of Zn(II)bis(3,4 dimethoxybenzoate)bis(nicotinamide) dihydrate, formulated as C 30 H 38 N 4 O 14 Zn, (I) has been obtained. According to experimental data, the complex can be characterized in the solid state as mononuclear, with a distorted octahedral stereochemistry. The distorted octahedral stereochemistry adopted by the complex was further confirmed by X-ray structure analysis of the current study, which consists of a six-coordinate Zn atom in a distorted octahedral environment constructed from two N atoms and four O atoms. The title compound crystallizes in the monoclinic space group C 2/c with a = 27.9248(18) Å, b = 8.5941(4) Å, c = 14.8344(11) Å, α = 90°, β = 108.651(5)°, γ = 90°, Z = 4. The molecular structure and geometry were also optimized using the B3LYP density functional theory method employing the 6-31G (d) basis set. Molecular electrostatic potential, frontier molecular orbital analysis, nonlinear optical properties and natural bond analysis for the title molecule are also described from the computational process.