- Simple Metal-Free Direct Reductive Amination Using Hydrosilatrane to Form Secondary and Tertiary Amines
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This work describes the use of cheap, safe, and easy-to-handle hydrosilatrane as the reductant in direct reductive amination reactions. This efficient method enables a facile, metal-free access to secondary and tertiary amines from a wide range of aldehydes and ketones, with the synthesis of tertiary amines requiring no additives at all. This reaction demonstrates excellent functional group tolerance, chemoselectivity, and scalability. (Figure presented.).
- Varjosaari, Sami E.,Skrypai, Vladislav,Suating, Paolo,Hurley, Joseph J. M.,Lio, Ashley M. De,Gilbert, Thomas M.,Adler, Marc J.
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supporting information
p. 1872 - 1878
(2017/06/09)
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- Synthesis and biological activity of some novel substituted quinazoline derivatives
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A new series of 4-N-(substituted benzyl)-2-phenyl-N-propylquinazolines were synthesized. The structures of the synthesized compounds were confirmed by IR, 1H NMR, 13C NMR and mass spectral analysis. All the synthesized compounds were screened for their analgesic and anti-inflammatory activity. Among the synthesized compounds 5c, 5h and 5o exhibited significant analgesic activity at 60 and 90 minutes reading, while compounds 5g, 5k and 5l exhibited significant anti-inflammatory activity at 3rd and 4th hr reading.
- Srivastav, Maneesh Kumar,Rajeeva,Salahuddin, Md.,Srinivasulu,Shanta Kumar
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p. 115 - 118
(2019/01/21)
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- Iridium-catalysed amine alkylation with alcohols in water
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Amines have been directly alkylated with alcohols using 1 mol% [Cp*IrI2]2 catalyst in water in the absence of base or other additives. The Royal Society of Chemistry 2010.
- Saidi, Ourida,Blacker, A. John,Farah, Mohamed M.,Marsden, Stephen P.,Williams, Jonathan M. J.
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supporting information; experimental part
p. 1541 - 1543
(2010/06/12)
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- HETEROCYCLIC DERIVATIVE HAVING INHIBITORY ACTIVITY ON TYPE-I 11 -HYDROXYSTEROID DEHYDROGENASE
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Disclosed is a compound which is useful as an 11β-hydroxysteroid dehydrogenase type 1 inhibitor. A compound represented by the formula: its pharmaceutically acceptable salt, or a solvate thereof, wherein X is O or S, a broken line and a wavy line represent the presence or the absence of a bond, (i) when a broken line represents the presence of a bond, a wavy line represents the absence of a bond, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, (ii) when a broken line represents the absence of a bond, a wavy line represents the presence of a bond, R1 and R4 are each independently hydrogen, halogen or the like, R2 and R3 are each independently hydrogen, halogen, cyano, hydroxy, carboxy, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like, and R5 and R6 are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl or the like.
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Page/Page column 135
(2010/08/07)
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- Preparation of benzolactams by Pd(OAC)2-catalyzed direct aromatic carbonylation
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We developed a new method for Pd(II)-catalyzed direct aromatic carbonylation in a phosphine-free catalytic system using Pd(OAc)2 and Cu(OAc)2 in an atmosphere of CO gas containing air. The carbonylation proceeded with ortho-palladation, inducing a remarkable site selectivity to afford a variety of five- or six-membered benzolactams from secondary ω-arylalkylamines, such as N-alkylbenzylamines or N-alkylphenethylamines. Copyright
- Orito, Kazuhiko,Horibata, Akiyoshi,Nakamura, Takatoshi,Ushito, Harumi,Nagasaki, Hideo,Yuguchi, Motoki,Yamashita, Satoshi,Tokuda, Masao
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p. 14342 - 14343
(2007/10/03)
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- Radical cyclisations of imines and hydrazones
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Radical cyclisation of sp3 carbon-centred radicals onto imines and hydrazones provides a new method for the synthesis of 5- and 6-membered ring nitrogen heterocycles. Cyclisation onto the electrophilic carbon of the C=N group and 5-exo stereoelectronic selectivity are the dominating mechanistic parameters. The C-centred radical intermediates were generated from benzeneselenyl precursors using Bu3SnH.
- Bowman, W. Russell,Stephenson, Peter T.,Terrett, Nicholas K.,Young, Adrian R.
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p. 7959 - 7980
(2007/10/02)
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- Generation of Aminyl Radicals using Sulfenamides as Synthetic Precursors
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Sulfenamides are synthesised from reaction between amines and N-(benzenesulfenil)-phthalimide or benzenesulfenyl chloride.The sulfenamides undergo reaction with tributyltin hydride to yield aminyl radicals which can be cyclised onto suitable alkenes. Key Words: sulfenamides; aminyl radicals; tributyltin hydride; radical-cyclisation; N-(benzenesulfenyl)phthalimide
- Bowman, W. Russell,Clark, David N.,Marmon, Robert J.
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p. 1275 - 1294
(2007/10/02)
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- Sulphenamides as synthetic precursors of aminyl radicals
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Sulphenamides, readily synthesised from reaction between benzenesulphenyl derivatives and amines, undergo facile reaction with radical generating reagents such as tributyltin hydride to yield aminyl radicals.
- Bowman, W.Russell,Clark, David N.,Marmon, Robert J.
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p. 6441 - 6444
(2007/10/02)
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