The four enantiopure diastereoisomers of β-hydroxy norvaline have been prepared from l-serine in moderate chemical yield. The method is based on the diastereoselective addition of different organometallics to easily accessible serinal derivatives.
N-ortho, meta and para-(ferrocenyl)benzoyl dipeptide esters 2–10 were prepared by coupling ferrocenyl benzoic acids 1 (ortho, meta and para) to the dipeptide ethyl esters GlyAbu(OEt) 2–4, GlyNva(OEt) 5–7 and GlyNle(OEt) 8–10 in the presence of N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide ...
Famotidine (3-([2-(diaminomethyleneamino) thiazol-4-yl] methylthio)-N′-sulfamoylpropanimidamide) is a histamine H2-receptor antagonist that inhibits stomach acid production, and it is commonly used in the treatment of peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD). Q...
3-exo-(Dimethylamino)isoborneol efficiently promotes the asymmetric addition of dialkylzincs to aldehydes. In order to characterize the catalytic organozinc species, relative reactivities of various substituted benzaldehydes and organozincs have been examined under enantiopure and racemic condit...
A series of organo-soluble polyimides were prepared from a novel fluorinated diamine monomer, 4-phenyl-2,6-bis[4-(4′-amino-2′-trifluoromethylphenoxy)phenyl]pyridine and various commercial aromatic dianhydrides. These polyimides had good solubility in common organic solvents. The obtained stron...
This article reports a simple and efficient synthesis of methyl(trifluoromethyl)oxaziridines, a new family of organic oxidizing agents. A detailed study on their oxygen transfer capability with respect to styrene, thioanisole and benzyl alcohol as model substrates for the synthesis of epoxides, ...
A new kind of pyridine-containing aromatic diamine monomer, 4-phenyl-2,6-bis[3-(4′-amino-2′-trifluoromethyl-phenoxy) phenyl] pyridine (m-PAFP), was successfully synthesized by a modified Chichibabin reaction of 3-(4′-nitro-2′-trifluoro-methyl-phenoxy)-acetophenone with benzaldehyde, followed...
A CuBr2-catalyzed alkylation of furans with a broad scope of benzyl alcohols and benzaldehydes is reported. Reaction proceeds efficiently under mild reaction conditions requiring no inert atmosphere or other precautions. Moreover, it is shown that CuBr2 catalyzes domino reactions of furans with ...
Monoclinic bismuth vanadate nanoparticles (nan-BiVO4) have been used for the selective photo-oxidation of benzyl alcohols (13 examples) to benzaldehydes under visible light irradiation using dioxygen as oxidant. Illumination with a blue LED (λmax = 470 nm) gave yields more than 30 times greater...
An efficient ‘on water’-promoted direct catalytic vinylogous addition of 3,5-dimethyl-4-nitroisoxazole to aldehydes and trifluoromethyl ketones was described, giving Henry (nitroaldol) adducts in excellent yields. The trifluoromethyl tertiary alcohol product could be transformed to the corresp...
Two chlorin derivatives bearing (trifluoromethyl)phenyl substituents at meso positions were synthesized via 1,3-dipolar cycloaddition. These pyrrolidine-fused chlorins are characterized by 1H, 13C NMR spectroscopy, mass spectrometry, UV-Vis absorption and fluorescence spectroscopy. The obtained ...
A novel class of imidazo[1,2-a]pyridines as melatonin receptor ligands is designed and synthesized. The affinities of 3-(6-methoxy-2-phenylimidazo[1,2-a]pyridine-3-yl)-N-methyl-propionamide 8, N-[2-(6-methoxy-2-phenylimidazo[1,2-a]pyridine-3-yl)-ethyl]-acetamide 13 and N-(1-hydroxy-3-(5-methoxy-...
Benzodiazepines and zolpidem are generally prescribed as sedative, hypnotics, anxiolytics or anticonvulsants. These drugs, however, are frequently misused in drug-facilitated crime. Therefore, a rapid and simple liquid chromatography–tandem mass spectrometric (LC–MS/MS) method was developed fo...
PurposeThe new analytical method of qualitative and quantitative determination of zolpidem and qualitative analysis of its main metabolite in blood and oral fluid samples was developed.
In order to investigate the influence of pigmentation on the incorporation of drugs into hair, time-course changes in drug distribution along non-pigmented (white) hairs as well as pigmented (black) hairs plucked from the same subject was observed following single administrations of two basic dr...
Zolpidem (ZPD) is an imidazopyridine hypnotic and little is known about the pharmacogenetics of ZPD. Our objective was to evaluate inter-individual genetic variation in conjunction with metabolic ratios of ZPD found in a toxicological analysis. Healthy individuals (n = 300) were genotyped for CY...
The aim of this study was to investigate the correlation between histories of zolpidem and benzodiazepines use and their concentrations in hair as determined by segmental hair analysis, that is, by analyzing hair samples taken 0–1, 1–2, 2–3, 3–4, 4–5, and 5–6 cm etc. and 0–3 cm from the s...
Zolpidem (ZPD) is an imidazopyridine derivative used as a new type of hypnotic and is commonly used in drug-facilitated crimes. A rapid, sensitive, and specific ultra-performance liquid chromatography–tandem mass spectrometry (UPLC/MS/MS) assay method for the simultaneous determination of zolpi...
Zolpidem (N,N-Dimethyl-2-[6-methyl-2-(4-methylphenyl)imidazo[1,2-a]pyridin-3-yl]acetamide) is a well-known drug for the treatment of sleeping disorders. Recent literature reports on positive effects of zolpidem therapy on improving renal damage after cisplatin and on reducing akinesia without sl...
We experienced a curious fatal case, in which a male in his 20s self-administered zolpidem intravenously. The victim was found dead lying on floor of his apartment room, with a tourniquet band and new injection marks on his right forearm. Nearby the body, a medical disposal syringe containing sm...
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