In continuation of our efforts to find new biologically active agents, regioselective synthesis of a series of 2-(3,5-dimethyl-1H-pyrazol-1-yl)-1-arylethanones 4a–k has been achieved under facile, extremely mild and greener reaction conditions with excellent yields. Moreover, one pot multicompo...
The novel complex of biologically active 3,3-dimethylglutarimide, aqua-bis(3,3-dimethylglutarimidato)mercury(II) has been obtained and its structure determined by single crystal X-ray diffraction and vibrational spectroscopic studies. The crystals of C14H20N2O4Hg·H2O are monoclinic, space group...
FT-Raman and FT-IR spectra are reported for 3,3-dimethylglutarimide, its N-deuterated derivative and the Hg(II) complex with 3,3-dimethylglutarimidate ion, Hg(C7H10NO2)2·H2O. A complete vibrational assignments are given for all internal vibrations of the molecules and are supported by normal co...
Ultrasonic velocity measurements, density measurements and viscometric studies were conducted for the drug buspirone hydrochloride (0.01–0.1 M) at three different concentrations (0.1, 0.05 and 0.025 M) at 298.15 K/1 atm. The buspirone hydrochloride was prepared in aqueous solutions of Cu(II) an...
The enantioselective microbial reduction of 6-oxo-8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione 1 to either of the corresponding (R)- or (S)-6-hydroxy-8-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-diones 2 and 3 is described.
The stereoselective synthesis of the title compounds has been performed. The relative configuration of methyl c-4-(tert-butoxycarbonylamino)-t-3-hydroxy-r-1-cyclohexanecarboxylate was confirmed by X-ray diffraction methods and its conformation in solution analyzed by NMR. The peptides containing...
Stereoselective synthesis of the title compounds was performed. The relative configuration of methyl t-4-(tert-butoxycarbonylamino)-c-3-hydroxy-r-1-cyclohexanecarboxylate and methyl trans-4-(tert-butoxycarbonylamino)-3-oxo-r-1-cyclohexanecarboxylate was confirmed by X-ray diffraction methods. An...
A photochemical decarboxylative cross-coupling reaction of aryl acetic acids with 1,4-dicyanobenzene (1,4-DCB) was developed. Under UV light irradiation, the inexpensive aryl acetic acids coupled with 1,4-DCB, isocyanates and alkene derivatives through decarboxylation which led to the correspond...
Aerobic granular sludge (AGS) has previously been utilized in the treatment of toxic compounds due to its diverse and dense microbial structure. The present study subjected mature AGS to model naphthenic acids (NAs) representative of the Canadian oil sands. To this effect, three NA concentration...
This report describes the behavior of four 1-amino-2-phenyl-1-cyclohexanecarboxylic acids, obtained in enantiomerically pure form starting from asymmetric Diels-Alder reactions between 1,3-butadiene and chiral (E)-2-cyanocinnamates, as chiral auxiliaries in the asymmetric Diels-Alder reactions o...
Hymenoic acid (1) is a natural compound isolated from cultures of a fungus, Hymenochaetaceae sp., and this structure was determined by spectroscopic analyses. Compound 1 is a novel sesquiterpene, trans-4-[(1′E,5′S)-5′-carboxy-1′-methyl-1′-hexenyl]cyclohexanecarboxylic acid. This compound se...
For the purpose of obtaining orally potent VLA-4 inhibitors, we have carried out structural modification of the (N′-phenylureido)phenyl group in compound 1, where the group was found to be attributed to poor pharmacokinetic profile in our previous research. Through modification, we have identif...
The microbial reduction of alpha-methyl, allyl and benzyl derivatives of alpha-acetyl-gamma-butyrolactones was carried out. It has been shown that different microorganisms, Kluyveromyces marxianus, Hansenula sp., Geotrichum candidum and Aspergillus niger, are capable to carry out the enantiospec...
The functionalized polyene 4′-[4,8-dimethyl-10-(2,6,6-trimethyl-1-cyclohexen-1-yl)-1,3,5,7,9-decapentaenyl]aniline has been synthesized from retinal and used to prepare [Mo(NO){HB(3,5-Me2C3N2H)3}Cl{HNC6H4-4-CHCHCHC(CH3)CHCHCHC(CH3)CHCHC9H15}], which does not exhibit detectab...
A series of N-methylthio-β-lactams with antibacterial activity were thoroughly evaluated as antioxidants. We found that only the presence of a polyphenolic moiety anchored to the β-lactam ring ensured an adequate antioxidant potency. New compounds, efficiently combining in one structure antiox...
An effective metal-free photoredox-mediated tandem addition/cyclization reaction of thiophenols or 1,2-diphenyldiselane with alkynes leads to 2,3-disubstituted benzothiophenes and benzoselenophenes. Blue light irradiation of the organic dye, Mes-Acr-Me+, initiates the photoredox catalysis. A ser...
A derivatization LC–MS/MS method was developed and qualified for the trace level quantification of 2-hydroxypyridine N-oxide (HOPO). HOPO is a coupling reagent used in the syntheses of active pharmaceutical ingredients (APIs) to form amide bonds. HOPO was recently confirmed to generate a positi...
Palladium catalyzed direct arylation of azine N-oxides using aryl triflates to afford the corresponding 2-aryl azine N-oxides is described. The reaction is carried out with a range of both N-oxides and aryl triflates. The arylation can be carried out in sequence to yield differentially diarylate...
N-Arylation of pyrrole with 3-iodo-4-methoxypyridine was investigated by copper catalysis under different conditions. The best conditions, that proved to be protocol A (CuI, DMEDA or TMEDA, K3PO4, DMF at 110 °C) and above all protocol B (Cu2O, Cs2CO3, DMSO at 110 °C), were applied to the synth...
The 2-hydroxypyridine-N-oxide derivative, 2- hydroxypyridine-N-oxide, 2,4-dihydroxypyeidine-N-oxide2-hydroxy -4-methoxypyridine-N-oxide and 2-hydroxy-4-(2′-methoxyethoxy)pyridine-N-oxide have been shown to remove iron from human transferrin and horse spleen ferritin at pH 7.4 at levels higher t...
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