An efficient and operationally simple method for the synthesis of β-keto sulfones through the BF·OEt-promoted reaction of alkynes and sodium sulfinates is developed. With its facile and selective access to the targets, it features good functional group compatibility, mild conditions, easily available starting materials, and good yields. Notably, the reaction does not require metal catalysts or chemical reagents with pungent odors.
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http://dx.doi.org/10.3390/molecules29153559 | DOI Listing |
Org Biomol Chem
December 2024
University College Dublin, School of Chemistry, Science Centre South, D04 N2E5 Dublin, Ireland.
The development of a continuous flow approach for the generation of alkynes from isoxazolones under diazotisation conditions is reported. The underlying transformation has been known for several decades; however, in batch mode, it is plagued by variable yields, excessive use of sodium nitrite and limited scalability due to its exothermic nature and the release of copious amounts of toxic nitroxide gases. The presented flow approach overcomes these limitations and delivers various alkyne products in residence times of less than 1 minute with productivities of 2 g h.
View Article and Find Full Text PDFChem Commun (Camb)
January 2025
Institute of Organic Chemistry and Biochemistry, Academy of Sciences of the Czech Republic, Flemingovo nám. 2, 160 00 Prague, Czechia.
Diazidodifluoromethane was prepared from dibromodifluoromethane, sodium azide and an alkanethiolate initiator. It represents the first example of a diazidomethane that is stable enough to be used in synthesis. The stability of (poly)azidomethanes was explored with calculations.
View Article and Find Full Text PDFACS Omega
November 2024
Helmholtz Institute for Pharmaceutical Research Saarland (HIPS)-Saarland University, Department of Pharmacy, Helmholtz Centre for Infection Research (HZI), Campus Building E8.1, 66123 Saarbrücken, Germany.
The enzyme IspE in is considered an attractive drug target, as it is essential for parasite survival and is absent in the human proteome. Yet it still has not been addressed by a small-molecule inhibitor. In this study, we conducted a high-throughput screening campaign against the IspE enzyme.
View Article and Find Full Text PDFAnal Chem
November 2024
Guangxi Key Laboratory of Green Processing of Sugar Resources, Department of Medicine, College of Biological and Chemical Engineering, Guangxi University of Science and Technology, Liuzhou 545006, Guangxi, P. R. China.
In this study, we developed ratiometric surface-enhanced Raman scattering (SERS) biosensors using Ag-Au alloy nanoflowers as SERS substrates, molecules having amide bonds and alkyne groups (Tag A) as Raman reporters, and sodium thiocyanate as an internal standard molecule (Tag B) for the sensitive detection of human carboxylesterase-1 (hCE1) in HepG-2 cells. The correlation between HepG-2 cell damage and hCE1 activity levels was investigated. Both Tag A's alkyne group and Tag B's cyanide group produced characteristic SERS signals in the Raman-silent region ( and , respectively).
View Article and Find Full Text PDFSci Rep
October 2024
Department of Chemistry, Faculty of Science, Ferdowsi University of Mashhad, Mashhad, Iran.
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