A simple and practical O2 oxidized scission of monosubstituted, gem- and 1,2-disubstituted, trisubstituted and tetrasubstituted aromatic olefins to aldehydes and ketones in PEGDME has been developed.
A direct arylsulfonylation of β,γ-unsaturated hydrazones method, in which sulfonated pyrazolines are accessed by a three-component reaction of β,γ-unsaturated hydrazones, DABSO, and aryldiazonium tetrafluoroborates, has been developed without external oxidants or catalysts. This transformation is triggered by the formation of arylsulfonyl radicals in situ from the reaction of aryldiazonium tetrafluoroborates and DABSO, and is enabled by controllable generation of C center radical, in which DABSO was utilized as the sulfone source and an oxidant in this radicalmediated cascaded reaction. A wide range of substrates can be applied in this process to afford pyrazolines in good yield, and it is amenable for gram-scale synthesis.
A simple, efficient, and clean approach for the synthesis of diverse dihydroisoquinolino[2,1-a]quinazolinones, 2-aryl quinazolinones, and analogues through intramolecular acceptorless dehydrogenative coupling has been achieved. The combination of bis(2-methoxyethyl)ether and molecular...
An oxidative 6-endo-trig cyclization and [2 + 2] cycloaddition of β,γ-unsaturated hydrazones/ketoximes and diazonium tetrafluoroborates for a synthetic strategy to pyridazin-4(1H)-ones/oxazin-4(1H)-ones under metal-free conditions is presented in a one-pot procedure. This protocol features excellent functional group tolerance and remarkable regioselectivity. A mechanistic study has been verified via 18 O labeling and the H 2 18 O labeling method, in which O 2 acts as both a reaction component and an oxidant. P yridazin-ones and oxazin-ones scaffolds, which contain two adjacent heteroatoms in the ring and one carbonyl group, are commonly found in a wide range of bioactive compounds, 1 pharmaceutical molecules, 2 functional materials, 3 and rarely natural products. 4 Among them, Pyridazin-4(1H)one and oxazin-4(1H)-one derivatives have gained tremendous attention because of their applications in the pharmacological properties such as antihypertensive, antinociceptive, antibacterial, antifungal, analgesic, anticancer, and inhibition activities (Figure 1). 5 However, due to the lack of suitable synthetic
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