- Stereoselective synthesis of quaternary benzylic carbons using C2 symmetric imidazolines and tetrahydrofuran as electrophile
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Alkylative ring opening of tetrahydrofuran in the presence of 9-BBN triflate is studied. Dianions derived from C2 symmetric imidazolines induce excellent to modest acyclic diastereoselectivity to form quaternary benzylic centers, using the 9-BBN triflate/THF system or methyl iodide as electrophiles. The direction of the stereoinduction is consistent in both cases. Absolute configuration for the newly created stereogenic center was established by chemical correlation. Low-temperature NMR studies of the dilithiated intermediates 42 and 43 suggest the presence of N- and C- metalated compounds, where the metal-bearing benzylic carbon is sp3 hybridized.
- Dalko, Peter I.,Langlois, Yves
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- Rapid synthesis and lipase inhibition activity of some new benzimidazole and perimidine derivatives
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This study presents a synthesis of new series of some benzimidazole, bisbenzimidazole and perimidine derivatives via microwave technique, which, leads to the good product yields and short reaction times. The structure of newly synthesized compounds was confirmed by 1H NMR and 13C NMR spectra. These compounds were screened for their lipase inhibition activity. Then, all compounds were evaluated with regard to pancreatic lipase activity, and some of the 2-substituted perimidines, bisperimidine and bisbenzimidazole derivatives showed lipase inhibition at various concentrations.
- Mente?e,Y?lmaz,Karaali,ülker,Kahveci
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p. 336 - 342
(2014/06/09)
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- Synthesis and choleretic activity of 3-[2-(3-R', 4-R'', 5-R'''-benzyl)-5- R-benzimidazol-1-yl]-butanoic acids
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On the ground of the evidentiated choleretic activity of 3-[2- benzylbenzimidazol-1-yl]butanoic acid, 28 new acids were prepared in order to evaluate the influence of suitable substitutions in either C5 of heteroring or C3', C4', C5' of benzyl group in po
- Grella,Paglietti,Sparatore,Satta,Manca,Peana
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- Synthesis and reactions of 2-amino-7,8-dimethoxy-1H-3-benzazepines. Competitive formation of 2-amino-1H-3-benzazepines VS. 2-benzylimidazoles
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A short synthesis of 2-amino-7,8-dimethoxy-1H-3-benzazepine (1a) from 3,4-dimethoxyphenylacetonitrile is reported. The synthesis of several other 2-amino-1H-3-benzazepines 1 is also discussed. Conditions which favor the formation of 1 versus the formation
- Robey,Copley-Merriman,Phelps
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p. 779 - 783
(2007/10/02)
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