New environmentally friendly solvent free synthesis of dihydropyrimidinones catalysed by N-butyl-N,N-dimethyl-α-phenylethylammonium bromide

N-Butyl-N,N-dimethyl-α-phenylethylammonium bromide catalyzes efficiently the three component condensation reaction of an aromatic aldehyde, a β-keto ester and urea/thiourea under solvent free conditions at 100°C to afford the corresponding dihydropyrimidinone in high yield.     

Millettia ferruginea extract attenuates cisplatin-induced alterations in kidney functioning,DNA damage,oxidative stress,and renal tissue morphology

This study aimed to investigate the beneficial role of Millettia ferruginea extract (MF) in preventing cisplatin (Cisp) induced nephrotoxicity in rats. A total of 55 metabolites were identified using LC-MS analysis. The in vivo results indicated that MF pretreatment for 4 weeks (20 mg/kg b.w.) remarkably attenuated the altered renal biomarkers by decreasing the levels of plasma creatinine, urea, and uric acid when compared to the Cisp-group. The nephroprotective capacity of MF was further strengthened by histopathological observations, where Cisp + MF treated rats showed lower number of inflammatory cells and tubular degenerative changes than the Cisp-group. The harmful effects of cisplatin on renal oxidative stress indicators (MDA, SOD, CAT, and GPx), were restored by the treatment of MF. In addition, the reduction of inflammatory markers (IL-6 and TNF-α), associated with alleviating DNA fragmentation, highlighted the preventive effect of MF in kidney tissue. Additionally, MF components presented lower binding energies when docked into the active site of TNF-α and IL-6. The present findings concluded that M. ferruginea extract exhibited nephroprotective potential, which may be attributed to its antioxidant and anti-inflammatory properties. Further work is recommended to confirm the current results, explore the involved mechanism of action, and determine the therapeutic doses and time.     

Polymer blends based on the β-modification of polypropylene

iPP/sPP, iPP/rPP, iPP/PVDF and iPP/PA-6 blends, and their β-nucleated forms were prepared in the present study. The components of iPP/sPP and iPP/rPP blends are compatible in the molten state. The phase structure of the melt of iPP/PVDF and iPP/PA-6 blends is heterogeneous. The melting and crystallisation characteristics as well as the structure and polymorphic composition of these blends were studied by polarised light microscopy (PLM) and differential scanning calorimetry (DSC). When semicrystalline polymers are added to iPP, the most important factor of the formation a blend with β-crystalline phase is the α-nucleation effect of the second polymer. In the case of polymers with an α-nucleating effect, the temperature range of their crystallisation should be lower than that of β-iPP. β-nucleated iPP/PVDF and iPP/PA-6 blends are extreme examples showing that completely β-iPP matrix can not form even in the presence of a highly effective β-nucleant, because of the strong α-nucleating ability and higher crystallisation temperature range of PVDF and PA-6. We found that the β-crystallisation tendency of random propylene copolymers can be enhanced by adding an iPP homopolymer.     

Reaction of a 5α-bromo-6β,19-epoxysteroid with BF3·Et2O/Ac2O: An evidence of a cyclic bromonium cation

Treatment of 3β-acetoxy-5-bromo-6β,19-epoxy-5α-androstan-17-one with Ac₂O and BF₃·OEt₂, produced the cleavage of the epoxy moiety and migration of the bromine atom to afford 3β,19-diacetoxy-6α-bromo-5-hydroxy-5β-androst-17-one in high yield.     

α-Tetralone glycosides from the green walnut husks of Juglans mandshurica Maxim. and their cytotoxic activities

Abstract

Five new α-tetralone glycosides, juglanbiosides A-E (1–5), together with an α-tetralone derivative (15) and nine known 1,4-naphthoquinones (6–14) were isolated from the 95% EtOH extract of green walnut husks of Juglans mandshurica Maxim. Their structures were elucidated by comprehensive spectroscopic methods (¹H, ¹³C NMR, DEPT, HSQC, HMBC, CD, HR-ESI-MS). In vitro cytotoxicities of all the isolated compounds were evaluated against BGC-823, HCT-15 and K562 cancer cell lines.

     

Synthesis of 2-(α-Hydroxyalkyl)-2-Oxazoline under Microwave Irradiation in Bluk

Four 2-(α-hydroxyalkyl)-2-oxazolines and a 2-(α-hydroxy-α,α-diphenyl)-2-benzooxazole were synthesized from β-amimoalcohols and α-hydroxy carboxylic acids under microwave irradiation in the absence of a solvent.     

TRIFLUOROMETHYLTHIOCOPPER CATALYZED OXIRANE RING OPENING

Trifluoromethylthiocopper has been found to catalyze the opening of the epoxide ring and to furnish not-so-easily accessible novel trifluoromethylthiolated α-hydroxy compounds. This communication presents the mechanism of the formation of the various compounds and their mass spectral data.     

Cyclohexanones--Source for Selena/Thiadiazoles and Diazaphospholes

Some new heterocyclic compounds containing selenadiazole, thiadiazole and diazaphosphole fused to cyclohexanones have been prepared and characterized by spectral data.     

Substitution of the Benzotriazolyl Group in N -(α-Amidoalkyl)benzotriazoles and N -(α-Sulfonamidoalkyl)benzotriazoles with Allylsamarium Bromide

Abstract

The nucleophilic substitution of the benzotriazolyl group in the N-(α-benzotriazol-1-ylalkyl)amides and N-(α-benzotriazol-1-ylalkyl) sulfonamides with allylsamarium bromide was investigated, and the corresponding homoallylamides or homoallylsulfonamides were obtained in good to excellent yields.     

The synthesis and physical evaluation of 5-alkoxy-1,3-thiazoles prepared via Lawesson's reagent-mediated cyclisation of α-benzamido esters

The synthesis of the first series of 5-alkoxy-1,3-thiazole-based liquid crystals is reported. The aforementioned liquid crystals were synthesised through a Lawesson's reagent-mediated cyclisation of appropriate α-benzamido esters. This methodology was found to be highly efficient, even on a large scale, and the resulting 5-alkoxy-1,3-thiazoles could be purified without the use of column chromatography. The synthesis and mesomorphic properties of a family of 5-alkoxy-2-(4-cyanophenyl)-1,3-thiazole liquid crystals prepared via this approach are discussed and compared with their thiophene and phenyl analogues.