- A concise approach to polysubstituted oxazoles from N-acyl-2-bromo enamides via a copper(i)/amino acid-catalyzed intramolecular C-O bond formation
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A straightforward and efficient copper(i)/amino acid-catalyzed intramolecular Ullmann-type C-O coupling reaction has been developed. This protocol affords a facile methodology for the synthesis of a series of novel 2,4,5-substituted oxazoles from readily accessible N-acyl-2-bromo enamides under mild conditions. This journal is the Partner Organisations 2014.
- Liu, Bingjie,Zhang, Yueteng,Huang, Gang,Zhang, Xinting,Niu, Pengfei,Wu, Jie,Yu, Wenquan,Chang, Junbiao
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p. 3912 - 3923
(2014/06/09)
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- Aminocarbonyl arylvinylbenzamides as gastric sparing anti-inflammatory agents
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Some (E/Z)-aminocarbonyl arylvinylbenzamides (B1-B15) were synthesized, evaluated for anti-inflammatory activity and ulcerogenic tendency, and their effect on gastro-intestinal motility in the rats was studied. These benzamides comprising of aliphatic unsaturated region situated between two amide linkages were synthesized by nucleophilic ring opening of appropriate azlactones (AZ1-AZ4) by suitable amines. The characterization of newly synthesized benzamides was performed by IR, 1H- and 13C-NMR, mass and elemental analysis. Amongst the tested compounds, benzamide B1, B2, B4, B5, and B13 were able to produce comparable or superior anti-inflammatory activity at 10 and 20 mg/kg p.o. dose with respect to standard diclofenac in carrageenan induced rat paw edema model with lessened propensity to cause gastro-intestinal hypermotility and were found to have nil tendencies to generate gastric ulcers. A series of N-[(E/Z)-2-(4-substituted/unsubstitutedphenyl)-1-{[arylamino] carbonyl} vinyl]benzamides (B1-B15) was synthesized by utilizing easily accessible starting material 4-substituted/unsubstituted benzylidene-2- phenyloxazol-5-one (AZ1-AZ4) and subjected to anti-inflammatory activity, gastrointestinal motility, and gastric damage studies in rats. Copyright
- Khadse, Saurabh C.,Talele, Gokul S.,Agrawal, Surendra S.
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experimental part
p. 292 - 300
(2011/11/05)
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- Synthesis and pro-kinetic activity of novel substituted aminocarbonyl arylvinylbenzamides
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Synthesis of benzamides (B1-B8) and their effect on gastrointestinal motility (prokinetic activity) in the rats is being reported in this paper. The compounds were characterized by spectral analysis (IR, NMR & Mass).
- Khadse,Talele,Agarwal
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experimental part
p. 277 - 280
(2011/12/14)
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