A simple, effective, and direct alkylation and acylation of indazoles using aldehydes under metal-free conditions has been developed. This regioselective alkylation/acylation protocol can proceed under mild conditions, tolerate a wide range of functional groups, and deliver multifunctional 2H-indazole derivatives with high efficiency. Mechanism studies indicated that a radical process was involved.
A copper-mediated oxidative functionalization of C(sp)-H bonds with isoquinolines via a radical process without ligands was achieved. The present system exhibits a novel pathway for the preparation of N-alkyl (benzyl) isoquinolin-1(2H)-ones in moderate to high yields. In addition, this procedure provides a simple method to afford 5-oxaprotoberberinones and their derivatives in two steps.
An effective approach to realize
the direct hydroxyalkylation of
imidazo[1,2-a]pyridines with alcohols promoted by
di-tert-butyl peroxide was described without any
metal catalyst. It is the first time that the dehydrogenative C(sp3)–C(sp2) coupling of imidazo[1,2-a]pyridines with alcohols occurred regioselectively at the
C-5 position of imidazo[1,2-a]pyridines. Multisubstituted
imidazopyridine derivatives were smoothly synthesized in moderate
to good yields. Through a series of control experiments, a free-radical
pathway was proposed to explain the experiment.
Eight novel silicon-containing diorganotin complexes with salicylaldehyde thiosemicarbazone were synthesized. They were characterized by 1 H NMR, 13 C NMR, IR spectra, elemental analysis and X-ray singlecrystal diffraction. Spectroscopic and X-rays studies indicated that the thiosemicarbazone Schiff base and tin atom were coordinated as a parallel five-and six-membered heterocyclic structure. In addition, the bioassay of the synthesized complexes was performed and the results show that the silicon-containing diorganotin complexes with salicylaldehyde thiosemicarbazone have good anticancer activity on human breast cancer cells.
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