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Now showing items 21-30 of 151
Selective C(sp2)−H Halogenation of "click" 4-Aryl-1,2,3-triazoles
(American Chemical Society, 2017-02-09)
Selective bromination reactions of “click compounds” are described. Electron-neutral and electron-deficient arenes selectively undergo unprecedented Pd-catalyzed C–H ortho-halogenations assisted by simple triazoles as ...
Exploring the Surface of the Ectodomain of the PD-L1 Immune Checkpoint with Small-Molecule Fragments
(American Chemical Society, 2022-09-08)
Development of small molecules targeting the PD-L1/PD-1 interface is advancing both in industry and academia, but only a few have reached early-stage clinical trials. Here, we take a closer look at the general druggability ...
Triazole-Directed Pd-Catalyzed C(sp2)–H Oxygenation of Arenes and Alkenes
(ACS Publications, 2016-02-24)
Selective Pd-catalyzed C(sp2)–H oxygenation of 4-substituted 1,2,3-triazoles is described. Unlike previous metal-catalyzed C–H functionalization events, which preferentially occur at the activated heterocyclic C–H bond, ...
Site-Selective Aqueous C–H Acylation of Tyrosine-Containing Oligopeptides with Aldehydes
(RSC, 2020-10-06)
The development of useful synthetic tools to label amino acids within a peptide framework for the ultimate modification of proteins in a late-stage fashion is a challenging task of utmost importance within chemical biology. ...
Site-Selective Trifluoromethylation Reactions of Oligopeptides
(Wiley, 2020-06-08)
Site-selective chemical modifications that target proteinogenic amino acid residues complement the methods entailing genetic manipulation, thereby allowing straightforward and rapid access to engineered proteins. The ...
Metal-catalyzed C–H functionalization processes upon “click”-triazole assistance
(Wiley, 2018-08-24)
The functionalization of otherwise unreactive C–H bonds holds great promise for reducing the reliance on existing functional groups while improving energy efficiency and atom-economy. One of the most powerful strategies ...
Pd-catalyzed site-selective C(sp(2))-H radical acylation of phenylalanine containing peptides with aldehydes
(Royal Society of Chemistry, 2019-08-07)
The site-selective functionalization of C-H bonds within a peptide framework remains a challenging task of prime synthetic importance. Herein, the first Pd-catalyzed delta-C(sp(2))-H acylation of Phe containing peptides ...
Pd-catalyzed site-selective C(sp2)–H radical acylation of phenylalanine containing peptides with aldehydes
(Royal Society of Chemistry, 2019-10-14)
The site-selective functionalization of C-H bonds within a peptide framework remains a challenging task of prime synthetic importance. Herein, the first Pd-catalyzed delta-C(sp(2))-H acylation of Phe containing peptides ...
Metal-Catalyzed C(sp2)−H Functionalization Processes of Phenylalanine- and Tyrosine-Containing Peptides
(Wiley, 2021-08-06)
The site-selective chemical diversification of biomolecules constitutes an unmet challenge of capital importance within medicinal chemistry and chemical biology. The functionalization of otherwise unreactive C-H bonds holds ...
Chiral gold(I) vs chiral silver complexes as catalysts for the enantioselective synthesis of the second generation GSK-hepatitis C virus inhibitor
(Beilstein Institut, 2011-07)
The synthesis of a GSK 2(nd) generation inhibitor of the hepatitis C virus, by enantioselective 1,3-dipolar cycloaddition between a leucine derived iminoester and tert-butyl acrylate, was studied. The comparison between ...