- Metal complexes of tosyl sulfonamides: Design, X-ray structure, biological activities and molecular docking studies
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The present study reports the synthesis of Zn(ii) complexes of tosyl sulfonamide derivatives obtained by the reaction of tosyl chloride with l-amino acids. The ligands and their complexes were characterized by IR, 1H and 13C-NMR, GC-
- Khan, Najm Ul Hassan,Zaib, Sumera,Sultana, Kishwar,Khan, Imtiaz,Mougang-Soume, Berline,Nadeem, Humaira,Hassan, Mukhtiar,Iqbal, Jamshed
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- Synthesis of α-amino acids by reaction of aziridine-2-carboxylic acids with carbon nucleophiles
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A variety of homochiral α-amino acids have been prepared in good yield via regioselective reaction of higher order cuprates with (2S)-N-para-toluenesulfonylaziridine-2-carboxylic acid 4. The reaction was much less regioselective and low yielding when higher order cuprates were reacted with the more hindered aziridine carboxylic acid 30, the principal products being protected β-amino acids. Reaction of lithium trimethylsilylacetylide with the aziridine acid 30, however, gave a protected α-amino acid which was converted to the protected isoleucine ester 37. The Royal Society of Chemistry 2006.
- Beresford, Kenneth J. M.,Church, Nicola J.,Young, Douglas W.
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p. 2888 - 2897
(2008/02/08)
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- Enzymatic approach to both enantiomers of N-Boc hydrophobic amino acids
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Protease catalysed hydrolysis of N-Boc-amino acid esters allows us to obtain N-Boc l-acids and d-esters of amino butanoic acid, nor-leucine, nor-valine, leucine and t-leucine in excellent ee. The reaction occurs in short reaction times and high concentrations. When a biphasic system (buffer-MTBE) is employed, a strong solvent effect is observed. This method could be of significance for the preparation of d-t-leucine, for which a practical method is currently unavailable.
- Agosta, Eleonora,Caligiuri, Antonio,D'Arrigo, Paola,Servi, Stefano,Tessaro, Davide,Canevotti, Renato
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p. 1995 - 1999
(2007/10/03)
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- PROCESS FOR MAKING N-SULFONATED-AMINO ACID DERIVATIVES
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This invention relates to a process for preparing optically active α -amino acid substrates which are used to make potent lethal factor (LF) inhibitors for the treatment of anthrax. This invention further relates to a process for synthesis of potent LF-inhibitors for the treatment of anthrax. Specifically, the invention concerns a novel, high-yielding and highly enantioselective asymmetric hydrogenation reaction of a tetrasubstituted ene-sulfonamide acid or ester.
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Page/Page column 24-25
(2008/06/13)
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- Peptidyl aldehyde inhibitors of calpain incorporating P2-proline mimetics
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Four new peptidyl aldehydes bearing proline mimetics at the P2-position were synthesized and studied as inhibitors of calpain I, cathepsin B, and selected serine proteases. The ring size of the P2-constraining residue influenced the
- Donkor, Isaac O.,Korukonda, Rajani,Huang, Tien L.,LeCour Jr., Louis
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p. 783 - 784
(2007/10/03)
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- Aldehyde derivatives and their use as calpain inhibitors
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Aldehyde derivatives with a specific calpain inhibiting activity and a platelet-aggregation inhibiting effect with formula (I) or formula (II): wherein R1 represents an aromatic hydrocarbon group, a heterocyclic group, or a group of-X-R3 in which X represents O,-S(O)m-(m = 0, 1, or 2), and R3 represents an aromatic hydrocarbon group, a heterocyclic group, or an alkyl group; Z represents R?-Y-or R?O-CH(R?)-in which Y represents a 3-to 7-membered nitrogen-containing saturated heterocyclic group, or a single cyclic saturated hydrocarbon group, R? represents an alkyl group, an alkenyl group, an alkynyl group, an acyl group, a sulfonyl group, an alkoxycarbonyl group, a carbamoyl group, or a thiocarbamoyl group, R? represents hydrogen, an alkyl group, or an aromatic hydrocarbon group, and R? represents an acyl group, a carbamoyl group, a thiocarbamoyl group, or an alkyl group; and n is an integer of 1 to 5. wherein R?, R?, R?, and R1? are defined in the specification.
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- An efficient preparation of optically active α-furfuryl amide by kinetic resolution using the modified sharpless asymmetric epoxidation reagent
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Kinetic resolution of α-furfuryl amide was first carried out by using the modified Sharpless asymmetric epoxidation reagent to give the slow-reacting enantiomers, (S)-la-f and (R)-lb,f in high enantioselectivity (90-100% e.e) and high chemical yield (45-5
- Zhou, Wei-Shan,Lu, Zhi-Hui,Wang, Zhi-Min
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p. 1467 - 1470
(2007/10/02)
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