Three of the 10 patients with SCI who were directly injected with autologous MSCs showed improvement in the motor power of the upper extremities and in activities of daily living, as well as significant magnetic resonance imaging and electrophysiological changes during long-term follow-up.
Transition-metal-catalyzed or metal-free azide-alkyne cycloadditions are methods to access 1,4- or 1,5-disubstituted 1,2,3-triazoles. Although the copper-catalyzed cycloaddition to access 1,4-disubstituted products has been applied to biomolecular reaction systems, the azide-alkyne cycloaddition to access the complementary 1,5-regioisomers under aqueous and ambient conditions remains a challenge due to limited substrate scope or moisture-/air-sensitive catalysts. Herein, we report a method to access 1,5-disubstituted 1,2,3-triazoles using a CpNi/Xantphos catalytic system. The reaction proceeds both in water and organic solvents at room temperature. This protocol is simple and scalable with a broad substrate scope including both aliphatic and aromatic substrates. Moreover, triazoles attached with carbohydrates or amino acids are prepared via this cycloaddition.
Synthesis
of sulfamoyl [18F]fluorides has been a challenging
topic owing to the inefficient nucleophilic radiofluorination of sulfamoyl
derivatives. Herein, we report an 18F/19F isotopic
exchange approach to synthesize various sulfamoyl [18F]fluorides,
otherwise inaccessible via direct synthesis from amines, with high
radiochemical yields up to 97% (30 examples). This late-stage labeling
protocol offers an efficient route to yield functionalized molecules
by diversifying the chemical library possessing sulfamoyl functionalities
through nucleophilic 18F incorporation within nitrogen-containing
sulfur(VI) frameworks.
Sulfuryl fluoride gas is a key reagent
for SO2F transfer.
However, conventional SO2F transfer reactions have limited 18F-radiochemistry translation, due to the inaccessibility
of gaseous [18F]SO2F2. Herein, we
report the first SO2F2-free synthesis of aryl
[18F]fluorosulfates from both phenolic and isolated aryl
imidazylate precursors with cyclotron-produced 18F–. The radiochemical yields ranged from moderate to
good with excellent functional group tolerance. The reliability of
our approach was validated by the automated radiosynthesis of 4-acetamidophenyl
[18F]fluorosulfate.
Annulative π-extension
chemistry provides a concise synthetic route to polycyclic arenes.
Herein, we disclose a nondirected annulation approach of unactivated
simple arenes. The palladium-catalyzed 2-fold C–H arylation
event facilitates tandem C–C linkage relays to furnish fully
benzenoid triphenylene frameworks using cyclic diaryliodonium salts.
The inseparable regioisomeric mixture of 1- and 2-methyltriphenylenes
is identified by the combined analysis of ion mobility-mass spectrometry,
gas-phase infrared spectroscopy, and molecular simulation studies.
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