- Iron-Catalysed Reductive Amination of Carbonyl Derivatives with Ω-Amino Fatty Acids to Access Cyclic Amines
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An efficient method for the reductive amination of carbonyl derivatives with ω-amino fatty acids catalysed by an iron complex Fe(CO)4(IMes) [IMes=1,3-bis(2,4,6-trimethylphenyl)imidazol-2-ylidene] by means of hydrosilylation was developed. A variety of pyrrolidines, piperidines and azepanes were selectively synthesised in moderate-to-excellent yields (36 examples, 47–97 % isolated yield) with a good functional group tolerance.
- Wei, Duo,Netkaew, Chakkrit,Carré, Victor,Darcel, Christophe
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p. 3008 - 3012
(2019/05/15)
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- Lysine-Based α-Peptide/β-Peptoid Peptidomimetics: Influence of Hydrophobicity, Fluorination, and Distribution of Cationic Charge on Antimicrobial Activity and Cytotoxicity
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Multidrug-resistant bacteria pose a serious threat to public health worldwide. Previously, α-peptide/β-peptoid hybrid oligomers were found to display activity against Gram-negative multidrug-resistant bacteria. In the present work, the influence of hydrop
- Molchanova, Natalia,Hansen, Paul R.,Damborg, Peter,Nielsen, Hanne M.,Franzyk, Henrik
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supporting information
p. 312 - 318
(2017/03/01)
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- Antimicrobial activity of peptidomimetics against multidrug-resistant Escherichia coli: A comparative study of different backbones
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Novel remedies in the battle against multidrug-resistant bacterial strains are urgently needed, and one obvious approach involves antimicrobial peptides and mimics hereof. The impact of α- and β-peptoid as well as β3-amino acid modifications on the activity profile against β-lactamase-producing Escherichia coli was assessed by testing an array comprising different types of cationic peptidomimetics obtained by a general monomer-based solid-phase synthesis protocol. Most of the peptidomimetics possessed high to moderate activity toward multidrug-resistant E. coli as opposed to the corresponding inactive peptides. Nevertheless, differences in hemolytic activities indicate that a careful choice of backbone design constitutes a significant parameter in the search for effective cationic antimicrobial peptidomimetics targeting specific bacteria.
- Jahnsen, Rasmus D.,Frimodt-M?ller, Niels,Franzyk, Henrik
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p. 7253 - 7261
(2012/11/07)
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- Thermophysical study of several α- And β-amino acid derivatives by differential scanning calorimetry (DSC)
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The present study reports a differential scanning calorimetry (DSC) study of the amino acids sarcosine [CAS Registry No. 107-97-1], α-alanine (dl) [CAS Registry No. 302-72-7], β-alanine [CAS Registry No. 107-95-9], N-benzyl-α-alanine (dl) [CAS Registry No
- Roux, Maria Victoria,Notario, Rafael,Segura, Marta,Guzman-Mejia, Ramon,Juaristi, Eusebio,Chickos, James S.
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experimental part
p. 3807 - 3812
(2012/05/21)
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- PARAKERATOSIS INHIBITOR, PORE-SHRINKING AGENT AND EXTERNAL COMPOSITION FOR SKIN
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The invention provides a parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent that has a function such as parakeratosis inhibition, pore shrinkage, or rough skin -inhibition/abatement, poses no safety problems such as sensory irritation, and is very safe, and further provides an external composition for skin to which a compound having the above-mentioned function has been added. The parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent comprises one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof. The external composition for skin comprises the one or more compounds selected from the group consisting of β-alanine derivatives and salts thereof as the above-mentioned parakeratosis inhibitor, pore-shrinking agent, or rough skin preventing/amaliorating agent.
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Page/Page column 22-23
(2008/06/13)
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- WRINKLE-IMPROVING AGENT
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The invention provides a novel wrinkle-improving agent that has an effect of improving wrinkles, that does not entail problems of safety or pain even when applied to the skin, and that contains a very safe substance as an active component. A discovery was made that N-benzoyl-β-alanine, other specific β-alanine derivatives, and salts thereof have a wrinkle-improving effect, whereby a wrinkle-improving agent containing as an active component one, two, or more types of compounds selected from the group composed of these specific β-alanine derivatives and the salts thereof was developed.
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- Natural phosphate modified with lithium nitrate: A new efficient catalyst for the construction of carbon-carbon, carbon-sulfur, and carbon-nitrogen bonds
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The addition of small amounts of lithium nitrate to natural phosphate followed by calcination gives a new catalyst Li/NP (weight ratio LiNO3/NP = 1/15). This material showed catalytic activity in the Michael addition of amines, mercaptans, and active methylene compounds to chalcone derivatives with high yields under mild reaction conditions. Li/NP is used as the catalyst for a facile synthesis of -amino acids, -sulfur acids, and 4 H-chromenes under heterogeneous conditions. The usual, undesirable byproducts from the Michael condensation such as 1,2-addition, bis-addition, and polymerization compounds are not observed with this method. The work-up procedure is simplified by simple filtration with the use of Li/NP.
- Zahouily, Mohamed,Mounir, Bahija,Cherki, Hind,Bahlaouan, Bouchaib,Rayadh, Ahmed,Sebti, Said
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p. 1203 - 1217
(2008/02/02)
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- Natural phosphate and potassium fluoride doped natural phosphate: Efficient catalysts for the construction of a carbon-nitrogen bond
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The application of natural phosphates doped with potassium fluoride as heterogeneous catalysts for the Michael addition of aromatic and aliphatic amines to α,β-unsaturated carbonyl compounds is presented. The natural phosphate catalyst can be regenerated and reused without loss of activity, which makes it an attractive alternative to homogeneous basic reagents. Doping natural phosphate with potassium fluoride significantly enhances the rate and yield of the reaction.
- Zahouily, Mohamed,Bahlaouan, Bouchaib,Rayadh, Ahmed,Sebti, Sa?d
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p. 4135 - 4138
(2007/10/03)
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- A convenient preparation of 1,3-disubstituted dihydro-2,4-(1H,3H) pyrimidinediones
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The ureas 3 which are obtained from 3-(benzylamino)propanenitrile (1) and various isocyanates (2) cyclize readily upon heating in ethanol, in the presence of hydrochloric acid, to form 3-substituted 1-benzyldihydro-2,4-(1H,3H)pyrimidinediones (11) in good
- Deck,Papadopoulos
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p. 675 - 680
(2007/10/03)
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- Catalyse intramoleculaire de l'aminolyse d'heterocycles phosphores derives des α aminoamides. I: Synthese de (thio) phosphor(N)diamides incorporant un residu de ss aminoacide
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A general scheme of intramolecular nucleophilic catalysis of aminolysis of the heterocycles B is proposed (Figure 2). The requisite heterocycle D, when built with a β aminoamide residue, allows also a repetitive β peptide synthesis, as with α aminoacids (Figure 1). In order to evaluate the feasibility of both schemes, fifteen phosphor(n)diamides (table III) incorporating one residue of β aminoacid, in form of esters 3, acids 5 (models of E, Figure 2), nitrile 11, or hydrazides 12 have been synthesized starting from P(IV) dichlorides 1 (Figure 3). Unexpectedly hydrolysis of nitriles 6 b c leads to β diacids 9 b c with the regular acids 8 b c.
- Dujols, Frederic,Jollet, Philippe,Mulliez, Michel
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p. 231 - 254
(2007/10/03)
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