Journal ArticleDOI
Rapid chromatographic technique for preparative separations with moderate resolution
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Abstract:
(11) Potassium ferricyanide has previously been used to convert w'c-1,2-dicarboxylate groups to double bonds. See, for example, L. F. Fieser and M. J. Haddadln, J. Am. Chem. Soc., 86, 2392 (1964). The oxidative dldecarboxylation of 1,2-dlcarboxyllc acids is, of course, a well-known process. See Inter alia (a) C. A. Grob, M. Ohta, and A. Weiss, Helv. Chim. Acta, 41, 1911 (1958); and (b) E. N. Cain, R. Vukov, and S. Masamune, J. Chem. Soc. D, 98 (1969).read more
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Cyclic pentapeptides as models for reverse turns: determination of the equilibrium distribution between type I and type II conformations of Pro-Asn and Pro-Ala β-turns
TL;DR: Comparing the conformational behavior of two peptides shows that both type I and type II β‐turns are present in equilibrium in these peptides, and preliminary assessment of the possible side‐chain/backbone conformations that contribute to the shift in populations is done.
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Synthetic Design for Combinatorial Chemistry. Solution and Polymer-Supported Synthesis of Polycyclic Lactams by Intramolecular Cyclization of Azomethine Ylides
TL;DR: An intramolecular version of the azomethine ylide cycloaddition reaction which utilizes readily available amino acids, aldehydes, and 2° amines as inputs is explored and a synthetic strategy that would be amenable to solid-phase synthesis of these compounds is identified.
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α‐Alkylation of Amino Acids without Racemization. Preparation of Either (S)‐ or (R)‐α‐Methyldopa from (S)‐Alanine
TL;DR: The self-reproduction of a center of chirality was introduced in this article, where enantiomerically pure α-amino acids can be α-alkylated with retention or with inversion of configuration through pivaladehyde acetal derivatives.
Journal ArticleDOI
Novel sigma receptor ligands. Part 2. SAR of spiro[[2]benzopyran-1,4'-piperidines] and spiro[[2]benzofuran-1,4'-piperidines] with carbon substituents in position 3.
TL;DR: Among the reported compounds, 1'-benzyl-3,4-dihydrospiro[[2]benzopyran-1,4'-piperidine]-3-carbonitrile 5 represents the most potent s Sigma(1) receptor ligand with a K(i) value of 1.54 nM and a sigma(1)/sigma(2) selectivity ratio of 1030.
Journal ArticleDOI
Nitrosothiol esters of diclofenac: synthesis and pharmacological characterization as gastrointestinal-sparing prodrugs.
Upul K. Bandarage,Liqing Chen,Xinqin Fang,David S. Garvey,Alicia Glavin,David R. Janero,L. Gordon Letts,Gregory J. Mercer,Joy K. Saha,Joseph D. Schroeder,Matthew J. Shumway,S. William Tam +11 more
TL;DR: Nitrosothiol esters of diclofenac comprise a novel class of NO-donating compounds having therapeutic potential as nonsteroidal antiinflammatory agents with an enhanced gastric safety profile.