Clean heterocyclic synthesis in water： I2/KI catalyzed one-pot synthesis of quinazolin-4（3H）-ones

Oxidative cyclocondensation of o-aminobenzamide with various aldehydes in water using I2/KI as catalyst and oxidizing agent is carded out giving the corresponding quinazolin-4（3H）-ones 3a-n in good to excellent yields.     

Synthesis of four series of quinoline‐based heterocycles by reacting 2‐chloroquinoline‐3‐carbonitriles with various types of isocyanides

Four distinct sets of functionalized quinolines were synthesized by reacting 2‐chloroquinoline‐3‐carbonitriles with various types of isocyanides under appropriate conditions. The palladium‐catalysed reaction of less hindered aliphatic and aromatic isocyanides with 2‐chloroquinoline‐3‐carbonitriles yielded 2‐alkyl(aryl)‐1‐imino‐1H‐pyrrolo[3,4‐b]quinolin‐3(2H)‐one derivatives; however, the catalysed reaction of more hindered isocyanides such as tert‐butyl isocyanide produced the corresponding 3‐cyanoquinoline‐2‐carboxamides. Interestingly, chloroquinoline‐3‐carbonitriles reacted with ethyl isocyanoacetate in the presence of Cs₂CO₃ to generate imidazo[1,5‐a]quinoline derivatives; notably, tosylmethyl isocyanide under the same conditions formed unprecedented 2‐tosyl‐3‐cyanoquinolines.     

A patent review on efficient strategies for the total synthesis of pazopanib,regorafenib and lenvatinib as novel anti-angiogenesis receptor tyrosine kinase inhibitors for cancer therapy

Molecular Diversity - Angiogenesis is an important and interesting scientific subject in the area of malignant tumours. Current research importance and interest are directed in connection to blood...     

A DFT study of the degradation mechanism of anticancer drug carmustine in an aqueous medium

Structural Chemistry - Density functional theory calculations were carried out to study the degradation mechanism of anticancer drug carmustine in an aqueous medium. The calculations indicate that...     

Silica‐supported Cu(II)–quinoline complex: Efficient and recyclable nanocatalyst for one‐pot synthesis of benzimidazolquinoline derivatives and 2H‐indazoles

The synthesis, characterization and catalytic activity of a Cu(II) complex derived from 2‐oxoquinoline‐3‐carbaldehyde Schiff base supported on amino‐functionalized silica are reported. 3‐(1H‐Benzo[d]imidazol‐2‐yl)quinolines containing piperidine, morpholine and phenylpiperazine skeletons at the C‐2 position were formed in good to excellent yields via the one‐pot reaction of 2‐chloroquinoline‐3‐carbaldehyde, benzene‐1,2‐diamines and secondary amines in the presence of the nanocatalyst under mild conditions. Moreover, the nanocatalyst was found to be recyclable for up to seven runs without significant loss of activity. Also, a series of 2H‐indazoles were synthesized by the catalytic condensation of 2‐bromobenzaldehyde, sodium azide and primary amines.     

Novel design of recyclable copper(II) complex supported on magnetic nanoparticles as active catalyst for Beckmann rearrangement in poly(ethylene glycol)

Copper complex‐functionalized magnetic core–shell nanoparticles (Fe₃O₄@SiO₂‐Lig‐Cu) were prepared and characterized using various techniques. The activity of the new catalyst was tested for the Beckmann rearrangement. The reaction conditions allow for the conversion of a wide variety of aldoximes, including aromatic and heterocyclic ones, to amides in good to excellent yields. High efficiency, mild reaction conditions, easy work‐up, use of poly(ethylene glycol) as a green medium and simple purification of products are important advantages of this system. Moreover, the eco‐friendly heterogeneous nanocatalyst could be easily recovered from the reaction mixture using an external magnet and reused several times.     

Effect of indium addition on the structure and magnetic properties of YIG

In this work we report the structure and magnetic properties of a series of single-phase indium-substituted yttrium iron garnet (In-YIG) nanoparticles with nominal composition of Y₃In_xFe_5−xO₁₂ (x=0.1, 0.2, 0.3 and 0.4) prepared by conventional mixed oxide route. Based on XRD results, the lattice parameters of the samples increased with increase in In³⁺ content due to its larger ionic radius. Mössbauer results confirmed the substitution of In³⁺ for Fe³⁺ in [a] site of YIG structure. Further, the magnitudes of the magnetic hyperfine field (MHF) were seen to reduce due to indium substitution. Moreover, a rising trend was observed for saturation magnetization (M_S) of the samples with x>0.2 owing to the substitution of non-magnetic In³⁺ for Fe³⁺. However, the observed initial drop of M_S for the sample with x=0.2 compared to that with x=0.1 is possibly attributed to the dominance of spin canting over the net magnetization rise caused by In³⁺ in [a] sites.     

Synthesis of new tripodal Hantzsch 1,4-dihydropyridines under solvent-free condition and their conversion to the corresponding tripodal pyridines

A mixture of β-ketoester and tri-aldehydes in the presence of ammonium fluoride was converted to their corresponding tripodal 1,4-dihydropyridines under solvent-free condition with good yields. The obtained tripodal 1,4-dihydropyridines were also aromatized with oxone^®/NaNO₂/wet SiO₂ system under mild and heterogeneous conditions quantitatively.     

A DFT study of both the hydrolytic degradation and protonation of semustine in variation conditions of pH and interaction of drug with DNA nucleobases

Structural Chemistry - Semustine as an anti-cancer medicine is decomposed by hydrolysis under pH-dependent conditions, forming chlorocarbonium ion and interaction with nucleic acid molecules. This...     

Central composite design optimization of dispersive liquid–liquid microextraction based on solidification of organic drop for the determination of 5-hydroxymethyl-2-furfural in orange juice using high-performance liquid chromatography

A simple, rapid and inexpensive dispersive liquid–liquid microextraction based on solidification of organic drop combined with HPLC was developed for the extraction and determination of trace levels of 5-hydroxymethyl-2-furfural in fruit juice. Effect of variables such as extracting and dispersive solvent volume and pH were investigated simultaneously using experimental design. Under the optimum conditions, the calibration graph was linear in the range of 1?200 μg/L with the detection limit of 0.3 μg/L. The optimized method revealed a good precision with relative standard deviation of 2.2%.The performance of the method was evaluated for extraction and determination of 5-hydroxymethyl-2-furfural in orange juice sample.