- Hypervalent Iodine(III) Reagent Mediated Regioselective Cycloaddition of Aldoximes with Enaminones
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An efficient oxidative cycloaddition of enaminones with nitrile oxides generated in situ from respective aldoximes using hypervalent iodine reagents has been developed. Reactions of various aldoximes with enaminones in the presence of [hydroxy(tosyloxy)iodo]benzene involved the regioselective cycloaddition reaction resulting in the formation of the 3,4-disubstituted isoxazoles in moderate to good yields. Structures of several isoxazole products were confirmed by a single X-ray crystallography.
- Yoshimura, Akira,Jarvi, Melissa E.,Shea, Michael T.,Makitalo, Cody L.,Rohde, Gregory T.,Yusubov, Mekhman S.,Saito, Akio,Zhdankin, Viktor V.
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p. 6682 - 6689
(2019/11/02)
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- Inhibitors of c-Jun N terminal kinases (JNK) and other protein kinases
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The present invention provides compounds of formula I: 1where R1 is H, CONH2, T(n)—R, or T(n)—Ar2, n may be zero or one, and G, XYZ, and Q are as described below. These compounds are inhibitors of protein kinase, particularly inhibitors of JNK, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.
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- A novel synthesis of isoxazoles via 1,3-dipolar cycloaddition of nitrile oxides to acetyl acetone
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Nitrile oxides (2) isolated from the oxidative dehydrogenation of aldoximes (1) by chloramines-T react with acetyl acetone (3) to afford 4-acetyl-3-aryl-5-methyl isoxazoles (5) in good yield. All new compounds were characterized by IR, 1H NMR,
- Umesha,Kumar, K. Ajay,Rai, K. M. Lokanatha
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p. 1841 - 1846
(2007/10/03)
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