The intramolecular amination of N-(3-bromopyridin-2-yl)azaheteroarylamines and N-(2-chloropyridin-3-yl)azaheteroarylamines was investigated. In this way we unraveled the mechanism of the ring closure reaction in the auto-tandem amination (inter- and intramolecular Pd-catalyzed amination) of 2,3-...

New high complex polymeric structures containing metal chelate sequences alternating, through esteric bridges, with silane units were obtained. The azomethine of 2,4-dihydroxybenzaldehyde with 1,3-bis(aminopropyl)tetramethyldisiloxane has been synthesized and in situ complexed with copper (II), ...

Primary tert-alkyl amines represent analogues of amantadine, a fragment commonly linked to pharmacophoric groups to enhance biological activity. The preparation of primary tert-alkyl amines is considered to be a difficult problem. Four synthetic procedures, which have been previously reported fo...

One unknown impurity (Imp-II) during the analysis of laboratory batches of isoproterenol hydrochloride was detected in the level ranging from 0.04% to 0.12% by high performance liquid chromatography with UV detection. The unknown impurity structure was proposed as 4-[2-(propan-2-ylamino)ethyl]be...

This paper describes the use of unsaturated Weinreb amides as excellent substrates for the Heck reaction. Subsequent derivatization of the products with organometallic reagents allowed access to a variety of substituted vinyl ketones that could not have been prepared directly via Heck reaction o...

An unexpected reaction of aryl ketone with acetohydrazone of aromatic aldehyde via 1,2-di-enamine/di-iminium mechanism was discovered, leading to efficient synthesis of 1,3,5-triaryl-1,5-diketones in good to excellent yields.

A straightforward synthesis of a library of largely new 3-vinylindoles via a clean dehydrative coupling reaction between ketones and indoles has been developed. Highly stable, non-nucleophilic aryl(2-methylindol-3-yl)methylium salts have been used as efficient Lewis acid catalysts. The advantage...

A highly efficient, green and sustainable protocol for rhodium(III)-catalyzed C-H alkylation of heterocycles with allylic alcohols has been achieved, which affords a series of β-aryl ketones in high yields. The reaction proceeds smoothly in water under air, and works well with heterocycles such...

A convenient, efficient and cost-effective two-stage synthesis of benzyl (3R)-3-amino-2-oxo-1-pyrrolidinecarboxylate (2S,3S)-2,3-bis[(4-methylbenzoyl)oxy]butanediote (2:1) via a crystallisation-induced dynamic resolution process is reported.

Steady-state fluorometric studies have been performed on 2-(2′-hydroxy-5′-methylbenzoyl)-1,5-diphenylpyrrole (HMBDPP) in aqueous and aqueous β-cyclodextrin (β-CD) environments at ambient temperature. The fluorophore mostly shows a single emission in aqueous solution. Addition of β-CD to the...

A novel ligand bridged copper(II) coordination polymer, [Cu(HL)(NO3)]n has been synthesized by reacting 2-oxo-1,2-dihydroquinoline-3-carbaldehyde (2′-methylbenzoyl) hydrazone (H2L) with Cu(NO3)2·3H2O, and characterized by X-ray diffraction studies. The DNA interaction studies revealed that the...

The thioureidomethylation of the sodium enolate of 2-(4-methylbenzoyl)cyclohexanone 3 with N-(tosylmethyl)thiourea 1a or N-(azidomethyl)thiourea 2 in acetonitrile results in the unexpected formation of N-(4-methylbenzoyl)-N’-[(2-oxocyclohexyl)-methyl]thiourea 6, which was structurally character...

Chalcones are important intermediates in the biosynthesis of biologically active compounds such as flavonoids and their derivatives. In this paper, a new chalcone 2E-1-(2ʹ-Hydroxy-3ʹ,4ʹ,6ʹ-trimethoxyphenyl)-3-(phenyl)-prop-2-en-1-one (HYTPHENYL) was synthesized by the condensation reaction of Cl...

We perform a theoretical investigation about the excited state intramolecular proton transfer (ESIPT) reaction for a novel 2-(2-hydroxy-3,5-dimethyl-phenyl)-benzooxazole-5-carboxylicacid (HDPBC) system. The ultrafast excited state process is due to the low potential barrier, which should be the ...

Offering novel scaffolds targeting estrogen receptor creates huge necessity to overcome the evolving resistance developed by tumors. Structure-based drug design coupled with ring opening strategy of the steroids skeleton revealed the potential of indole-based analogs to be synthesized targeting ...

In this study, 3-(9-anthryl)-1-(3-hydroxyphenyl)prop-2-en-1-one was synthesized and formed two cis isomers (α and β polymorphs) and one trans isomer under different crystallization conditions. Single crystal X-ray diffraction revealed that all the three crystals exhibit the similar crystal str...

Neuropathic pain is a chronic pain caused by a lesion or disease affecting the somatosensory nervous system. To date, no specific treatment has been developed to cure this pain. Antidepressants and anticonvulsant drugs are used, but they do not demonstrate universal efficacy, and they often caus...

The binding of 5-iodouridine with human serum albumin was investigated under the simulative physiological conditions. The fluorescence spectra in combination with UV absorption and modeling method were used in the present work. A strong fluorescence quenching reaction of 5-iodouridine to HSA was...

An operationally simple, inexpensive, efficient, and environmentally friendly esterification of various carboxylic acids, phosphonic acids, and phosphinic acids with triethyl orthoacetate or trimethyl orthoacetate under neutral conditions in a typical room temperature ionic liquid, 1-butyl-3-met...

A series of 4-arylamido 3-methyl isoxazoles were synthesized and evaluated for their antiproliferative activities against the A375P melanoma and U937 hematopoietic cell lines. Most compounds showed selective antiproliferative activity toward the U937 cell line and the activities were better than...