Qingshan Zhang

A mild, efficient, and selective procedure for transprotection of acetonides to acetates catalyzed with HClO4-SiO2.

The transformation of acetonides into acetates is frequently required in synthetic chemistry. An efficient procedure for direct conversion of acetonides into acetates in the presence of HClO(4)-SiO(2) under mild conditions was developed. The acetonides of primary hydroxy groups are directly converted to diacetates, and the anomeric acetonides of furanosides are stereoselectively transformed into the corresponding acetyl beta-d-furanosides with a 2-acetoxyisopropyl group.

Synthesis and bioactivity of novel trisubstituted triazole nucleosides

ABSTRACT A series of novel trisubstituted 1,2,3-triazole purine nucleosides were efficiently synthesized via Huisgen 1,3-dipolar cycloaddition in good yields. Bioactivity against cytomegalovirus (CMV) and varicella-zoster virus (VZV) in human embryonic lung cell cultures was evaluated and all compounds show low antiviral activity.

A novel polyaspartic acid derivative with multifunctional groups for scale inhibition application

ABSTRACT Polyaspartic acid is a green biodegradable antiscalant and widely applied in water treatment field. However, its scale inhibition efficiency is not prominent, especially for calcium orthophosphate. So we introduced acylamino and hydroxyl groups simultaneously to prepare a novel polyaspartic-acid derivative (PASPTU) with multifunctional groups by the reaction of polysuccinimide with threonine and urea. The graft copolymer was analyzed by using nuclear magnetic resonance, gel permeation chromatography, thermogravimetric analyzer and Fourier transform infrared spectroscopy. Its scale inhibition performance for calcium orthophosphate, calcium sulfate and calcium carbonate was evaluated. The findings showed that the scale inhibition rates of the graft copolymer reached up to 100% for calcium orthophosphate, 100% for calcium sulfate and 91% for calcium carbonate at certain dosages. The findings above showed that the copolymer had excellent scale inhibition efficiency for calcium salts in water treatment processes.

Synthesis and Ativiral Activity of 5-(Benzylthio)-4-carbamyl-1,2,3-triazoles Against Human Cytomegalovirus (CMV) and Varicella-zoster Virus (VZV)

BACKGROUND All of the clinical drugs for herpesvirus infections exhibit high toxicity and suffer from significant drug-resistantance. There is a great need for the development of new, effective, and safe anti-herpesvirus agents with different mechanisms of action. METHODS A series of novel 5-(benzylthio)-1H-1,2,3-triazole-4-carboxamides were efficiently synthesized and EC50 values against human cytomegalovirus (HCMV), varicella-zoster virus (VZV) and herpes simplex virus (HSV) were evaluated in vitro. RESULTS Some compounds possess antiviral activity. Compound 7f exhibits promising inhibitory activity against both HCMV and VZV. Our results also indicate that these derivatives are independent of the viral thymidine kinase (TK) for activation, which is indispensable for current drugs. CONCLUSION 4,5-Bissubstiuted triazoles are active against herpesviruses and the nature and the position of substituents in the benzene ring remarkably affect their activity, such as bromo, cyano and cyanovynil substituents. Future studies should be undertaken to investigate the mechanism of action of these compounds.

(5S*,6R*,7R*)-6-Formyl-5-phenyl-7-propyl-perhydro-pyrazolo[1,2-a]pyrazol-1-one.

The title compound, C16H20N2O2, was obtained by catalytic asymmetric cycloaddition of trans-3-propylacrolein with 1-benzylidenepyrazolid-3-one betaine. There are two symmetry-independent molecules in the asymmetric unit. In both molecules, the two five-membered heterocyclic rings adopt envelope conformations.