- Novel one-step synthesis of thiazolo[3,2-b]1,2,4-triazoles.
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[reaction: see text] Reactions of chalcones 3a-f with bis(1H-1,2,4-triazolyl) sulfoxide 4 formed the thiazolo[3,2-b]1,2,4-triazoles 5a-f, which resemble closely some previously prepared COX-2 inhibitors. The structure of 5a was confirmed by X-ray analysis
- Katritzky,Pastor,Voronkov,Steel
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- A convenient approach to β-heteroarylated (C-N bond) ketones from Cs2CO3 promoted reaction between propargyl alcohols and nitrogen-heterocycles
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An efficient and direct approach to β-heteroarylated (C-N bond) ketones is demonstrated. Base promoted redox isomerization of propargyl alcohol to α,β-unsaturated ketone followed by conjugate addition to NH-heteroarenes affords a wide range of β-heteroarylated ketones in good to excellent yields. Aryl, heteroaryl, alkyl C(sp), and terminal alkynes containing unactivated propargyl alcohols effectively undergo redox-isomerization conjugate addition (RICA) with NH-heteroarenes. Reaction of 3-substituted pyrazoles or indazole with propargyl alcohols enables highly regioselective products. A diverse range of NH-bearing nucleophiles such as: pyrazoles, imidazole, triazoles, pyrrole, indoles and aniline participate in this reaction and deliver the corresponding β-heteroarylated ketones.
- Bhanuchandra,Kuram, Malleswara Rao,Sahoo, Akhila K.
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p. 3538 - 3555
(2012/05/20)
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- CHEMICAL COMPOUNDS
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Compounds of formula (I):wherein variable groups are as defined within; for use in the inhibition of 11betaHSD1 are described
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