- Synthesis and 2D QSAR of O-sulphonated β-aminols derivatives as novel antifungal and antibacterial agents
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Synthesis of a series of b-aminol derivatives using regioselective opening reaction catalyzed by SiO2 (60-120 mesh) and O-sulphonation in THF-KOH system, comprising tert-butoxycarbonyl at secondary nitrogen and evaluate for various stains of bacteria and fungi. SAR study of synthesized compound using backward regression analysis.
- Saxena, Anil K.,Sharma, Sugandha,Pandey, Atindra K.,Shukla, Praveen K.
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scheme or table
p. 6476 - 6481
(2011/11/29)
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- Weinreb amide based synthetic equivalents for convenient access to 4-aryl-1,2,3,4-tetrahydroisoquinolines
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New synthetic equivalents, N-methoxy-N-methyl-N′-phenylsulfonyl glycinamide and N-methoxy-N-methyl-N′-benzyl-N′-tert-butyloxy carbonyl glycinamide based on WA functionality were developed for the convenient synthesis of 4-aryl-1,2,3,4-tetrahydroisoquinoline framework. Two simple reactions, N-benzylation and addition of arylmagnesium halide on the WA functionality of the former afforded the key intermediate for convenient synthesis of N-phenylsulfonyl protected 4-aryl-1,2,3,4-tetrahydroisoquinoline, through reduction and acid promoted cyclization. With the latter, the addition of arylmagnesium halide on the WA functionality followed by the same protocol afforded the direct synthesis of 4-aryl-1,2,3,4-tetrahydroisoquinolines in good yields. The acid promoted cyclization step enabled concomitant removal of N-Boc protection.
- Kommidi, Harikrishna,Balasubramaniam, Sivaraman,Aidhen, Indrapal Singh
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experimental part
p. 3723 - 3729
(2010/07/05)
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- Enantioselective synthesis of β-hydroxy amines and aziridines using asymmetric transfer hydrogenation of α-amino ketones
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Enantioselective transfer hydrogenation of α-amino ketones is an effective method for the asymmetric synthesis of β-hydroxy amines and aziridines.
- Kawamoto,Wills
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p. 1916 - 1928
(2007/10/03)
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- Enantioselective synthesis of β-hydroxy amines and aziridines using asymmetric transfer hydrogenation of α-amido ketones
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A rapid, expedient and enantioselective method for the synthesis of β-hydroxy amines and monosubstituted aziridines in up to 99% e.e., via asymmetric transfer hydrogenation of α-amido ketones, is described. Copyright (C) 2000 Elsevier Science Ltd.
- Kawamoto, Aparecida,Wills, Martin
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p. 3257 - 3261
(2007/10/03)
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