- Chemoselective mono halogenation of β-keto-sulfones using potassium halide and hydrogen peroxide; synthesis of halomethyl sulfones and dihalomethyl sulfones
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The synthesis of α-halo β-keto-sulfones using potassium halide and hydrogen peroxide as a chemoselective mono halogenation reagent and the synthesis of α,α-symmetrical and asymmetrical dihalo β-keto-sulfones and α-halo, α-alkyl and β-keto-sulfones is described. Base induced cleavage of α-halo β-keto-sulfones, α,α-dihalo β-keto-sulfones, and α-halo, α-alkyl β-keto-sulfones afforded the corresponding halomethyl sulfones, dihalomethyl sulfones and haloalkyl sulfones.
- Suryakiran,Prabhakar,Srikanth Reddy,Chinni Mahesh,Rajesh,Venkateswarlu
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p. 877 - 881
(2007/10/03)
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- Rapid and convenient synthetic strategy for 2-amino-4-aryl-5-aryl-sulfonyl thiazoles
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Synthesis of 2-amino-4-aryl-5-arylsulfonyl thiazoles 2a-i have been successfully carried out in one pot by condensing α-aryl sulfonyl-4-substituted acetophenones with phenyl trimethyl ammonium tribromide (PTT) and thiourea. The required α-aryl sulfonyl-4-substituted acetophenones have also been prepared by modified one pot method.
- Bhingolikar,Mahalle,Bondge,Mane
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p. 2589 - 2593
(2007/10/03)
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- Mild Halogenation of Stabilized Ester Enolates by Cupric Halides
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The reactions of various stabilized ester enolates of 2-keto, 2-(alkoxycarbonyl), 2-phosphoryl, and 2-(benzenesulfonyl) esters with cupric chloride or cupric bromide have been examined.The reactions lead to 2-halo esters in good to excellent yields under mild condition.Enolates which contain an unsaturated functionality such as a double bond, a triple bond, or an allylic or a benzylic moiety react with high chemoselectivity.
- Shi, Xiao-Xin,Dai, Li Xin
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p. 4596 - 4598
(2007/10/02)
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- Effect of Structural Change on Acute Toxicity and Antiinflammatory Activity in a Series of Imidazothiazoles and Thiazolobenzimidazoles
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The effect of structural change on the biological activity of a series of imidazothiazoles and thiazolobenzimidazoles is described.It was found that compounds with polar substituents at the 2 or 3 position of the ring system are less acutely toxic while maintaining antiinflammatory activity.Other structural changes, such as the incorporation of a gem-dimethyl substituent in the 6 position, increase acute toxicity and eliminate antiinflammatory activity.The compound with the best activity/toxicity ratio contains an alkyl sulfonyl substituent on the thiazole ring.The thiazolobenzimidazole analogues are more potent than the imidazole analogues.
- Powers, Larry J.,Fogt, S. W.,Ariyan, Z. S.,Rippin, D. J.,Heilman, R. D.,Matthews, Richard J.
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p. 604 - 609
(2007/10/02)
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