Synthesis of flavones from 2'-allyloxy-α, β-dibromochalcones has been described. The iodine induced oxidative cyclization of 2'-allyloxy-α, β-dibromochalcones results into the formation of 3-bromoflavanones which ultimately gives flavones. Dehydrobromination of 3-bromoflavanone to give flavone is the preferred reaction over dehydrogenation.
A fast, mechanochemical and solvent-free synthesis of substituted tetrahydropyrimidines and octahydroquinazolines under Au(III)-catalysis has been developed. The practical feasibility, eco-friendliness and operational simplicity of this chemistry is exemplified by ball milling three components such as formaldehyde, amines and 2-butynedioates/dimedone in a shaker mill for as little as five minutes, thus avoiding the requirement of undesirable solvents and long reaction times. Moreover, this protocol furnishes the target compounds in high yields without any side products and in some cases offers products with excellent regioselectivity. Out of the 26 compounds screened for anticonvulsant potency, 11 compounds exhibited comparable activity against a standard drug.
A series of 2‐phenyl‐2,3‐dihydrochromon‐4‐one derivatives (flavanone derivatives) were synthesized by silica gel assisted isomerization of several α‐methyl‐2′‐hydroxy chalcones in 74%–88% yield. These flavanones were further oxidized to 3‐methyl flavones by using iodine in dimethyl sulphoxide at 60°C in presence of acid. The newly synthesized derivatives were evaluated for in vitro study against Staphylococcus aureus, Micrococcus luteus and Staphylococcus epidermis.
Pyrazole derivatives R 0180An Efficient Synthesis of 1-H Indazoles. -Salicyaldehydes and o-hydroxyacetophenone react with hydrazine hydrochloride or phenylhydrazine to afford the biologically important products. -(LOKHANDE*, P. D.; RAHEEM, A.; SABALE, S. T.; CHABUKSWAR, A. R.; JAGDALE, S. C.; Tetrahedron Lett. 48 (2007) 39, 6890-6892; Dep. Chem., Univ. Pune, Pune 411 007, India; Eng.) -Mais 03-117
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