- Hydroaminomethylation of Olefins with Aminomethyltrifluoroborate by Photoredox Catalysis
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A photocatalytic hydroaminomethylation of olefins with N-protected aminomethyltrifluoroborates has been developed. This methodology provides a new strategy for the introduction of a primary aminomethyl group onto electron-deficient C=C bonds. This reaction constitutes a facile entry into synthetically useful γ-aminobutyric acid (GABA) derivatives such as baclofen.
- Miyazawa, Kazuki,Koike, Takashi,Akita, Munetaka
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p. 2749 - 2755
(2016/02/18)
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- Direct stereospecific amination of alkyl and aryl pinacol boronates
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The direct amination of alkyl and aryl pinacol boronates is accomplished with lithiated methoxyamine. This reaction directly provides aliphatic and aromatic amines, stereospecifically, and without preactivation of the boronate substrate.
- Mlynarski, Scott N.,Karns, Alexander S.,Morken, James P.
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supporting information
p. 16449 - 16451,3
(2020/09/15)
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- HETEROCYCLIC MODULATORS OF PKB
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The invention relates to heterocyclic compounds of Formula I and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein Formula (I). The invention also relates to the therapeutic use of such compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
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Page/Page column 130-131
(2009/03/07)
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- Synthesis of 13C-dilabeled 4-coumaroylspermidines
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Five 13C-dilabeled constitution isomers of 4-coumaroylspermidines were prepared in nine to eleven steps: N1,4-di[(E)-4-coumaroyl]-(5,8- 13C2)spermidine (13b), N1-[(E)-4-coumaroyl]-(5,8-13C2)spermidine (17b), N1,8-di[(E)-4-coumaroyl]-(1,4-13C2)spermidine (20b), N4-[(E)-4- coumaroyl]-(1,4-13C2)spermidine (24b) and N1,4,8-tri[(E)-4-coumaroyl]- (5,8-13C2)spermidine (26). The two 13C-atoms were subsequently introduced using labeled potassium cyanide. The synthesis proceeds through stepwise construction of the polyamine backbone including protection and deprotection steps of the amino functions. Based on 1H-1H NOE interactions, the preliminary study of their binding reveals that 20b binds to tRNA in the same way as spermidine does, whereas 24b and 26 do not show any NOE effects with the tRNA protons.
- Geneste, Herve,Hesse, Manfred
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p. 15199 - 15214
(2007/10/03)
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- The Mass Spectral Loss of Water from Macrocyclic Amino-ketones
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Macrocyclic oxo-lactams containing an N-alkylamino side chain are stable natural products.Their electronimpact mass spectra are characterized by intensive >M - H2O>(1+) signals, the molecular ion signal itself is missing.Under electospray ionization condi
- Benz, Herbert,Hesse, Manfred
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p. 1636 - 1648
(2007/10/02)
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- A Convenient and General Method for the Preparation of tert-Butoxycarbonylaminoalkanenitriles and Their Conversion to Mono-tert-butoxycarbonylalkanediamines
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A new method is described for the synthesis of tert-butoxycarbonylaminoalkanenitriles 3 by dehydration of the corresponding carboxamides 2 (prepared in two steps from aminoalkanoic acids) in the presence of trifluoroacetic anhydride and triethylamine.N-Boc-aminoalkanenitriles 3 are easily converted to mono-N-Boc-alkanediamines 4 under mild conditions avoiding the cleavage of the N-protective group.The monoprotected alkanediamines 4 are useful tools in affinity chromatography.
- Houssin, Raymond,Bernier, Jean-Luc,Henichart, Jean-Pierre
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p. 259 - 261
(2007/10/02)
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- Tetrazole analogues of GABA-mimetic agents
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Six tetrazole analogues of GABA-mimetic compounds were synthesized. In vitro only two compounds, analogues of GABA and isoguvacine, showed a weak affinity for GABA-A and GABA-B receptors. In vivo compounds were inactive in a psychopharmacological screening in mice. The results were interpreted in terms of intercharge distance, electronic delocalisation and ability of membrane crossing.
- Schlewer,Wermuth,Chambon
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p. 181 - 186
(2007/10/02)
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