A direct
ring-opening/nucleophilic substitution reaction of N1-H-1,2,3-triazoles has been described. Divergent (Z)-β-halogen- or sulfonyl-substituted enamides could
be stereospecifically synthesized in a tunable manner. This strategy
might not only enable a new ring-opening method of N1-H-1,2,3-triazoles under nonmetal catalysis and mild reaction conditions
but also offer a good opportunity to reliably access versatile (Z)-β-substituted enamides that could be used as synthetic
precursors for further synthetic transformations.
Sulfur-containing heterocycles are important structural units that could be commonly found in pharmaceuticals and functional molecules. Herein, we report a cycloaddition reaction of 1,2,3-thiadiazoles with isonitriles to obtain 4,5-disubstituted thiazoles...
We here reported a direct ring-opening/semipinacol rearrangement reaction of 4-(1-hydroxycyclobutyl)-1,2,3-triazole, in which N-acyl substituted 1,2,3-triazole was generated in situ and would trigger thermodynamically controlled electrocyclization ring-opening to afford rearrangement precursor...
Nucleophilic
aromatic substitution (SNAr) reaction in
classic textbook is a stepwise mechanism, and few examples of concerted
reactions have been reported. Herein, we developed a concerted SNAr reaction of 5-bromo-1,2,3-triazines with phenols in which
the nonclassic mechanism of this reaction could be revealed by calculation.
Furthermore, the resulting 5-aryloxy-1,2,3-triazines could be used
as convenient precursors to access biologically important 3-aryloxy-pyridines
in one-pot manner.
Fabrication of self-delivery drug systems can surmount
low drug
bioavailability and achieve a precise therapeutic process. In this
study, a hydrogen sulfide-responsive (H2S) small molecule
prodrug was synthesized by linking two chemotherapy drugs, camptothecin
(CPT) and gemcitabine (GT), using a reductive disulfide bond simultaneously
with a lock GT strategy using a H2S-responsive azide group
(denoted as N3-GT-CPT). The ingenious design endows the
easy coprecipitation peculiarity of the prodrug with clinical indocyanine
green (ICG) via a combined interaction force of hydrophobic, π–π
stacking, and electrostatic interactions of anions and cations, thus
producing a more stable and multifunctional therapeutic nanosystem.
Considering the great photothermal and imaging ability of ICG, the
obtained nanosystem showed an excellent therapeutic ability against
colon tumors in vitro and in vivo with selective response to intercellular H2S, thus offering
a good combination-based multiple therapy for treatment of tumors.
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