Výsledky vyhledávání - "Johan J N, Veerman"

Discovery of 2,4-1H-Imidazole Carboxamides as Potent and Selective TAK1 Inhibitors

Publikováno v: ACS Medicinal Chemistry Letters. 12:555-562

Herein we report the discovery of 2,4-1H-imidazole carboxamides as novel, biochemically potent, and kinome selective inhibitors of transforming growth factor β-activated kinase 1 (TAK1). The target was subjected to a DNA-encoded chemical library (DE

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::4d65527e5f7e8fb6d40ba9c6dda27029
https://doi.org/10.1021/acsmedchemlett.0c00547

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Discovery of 2,4-1

Publikováno v: ACS Med Chem Lett

[Image: see text] Herein we report the discovery of 2,4-1H-imidazole carboxamides as novel, biochemically potent, and kinome selective inhibitors of transforming growth factor β-activated kinase 1 (TAK1). The target was subjected to a DNA-encoded ch

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https://pubmed.ncbi.nlm.nih.gov/33859795

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Synthesis of 2,6-Bridged Piperazine-3-ones by N-Acyliminium Ion Chemistry

Autor: Floris P. J. T. Rutjes, Johan J. N. Veerman, Jan H. van Maarseveen, Robin S. Bon, Henk Hiemstra, Daniel Girones, Bui T. B. Hue

Publikováno v: Journal of Organic Chemistry, 68, 4486-4494. American Chemical Society

Several 2-substituted and 2,5-disubstituted piperazine-3,6-diones were synthesized starting from readily available alpha-amino acids. After activation of a lactam carbonyl via introduction of a methoxycarbonyl group onto nitrogen, this carbonyl was s

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https://doi.org/10.1021/jo0342572

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Solid-Phase Synthesis of Piperidines by N-Acyliminium Ion Chemistry

Autor: Floris P. J. T. Rutjes, Jasper Klein, Henk Hiemstra, Johan J. N. Veerman, Hans W. Scheeren, Jan H. van Maarseveen, René W. M. Aben, Chris G. Kruse

Publikováno v: European Journal of Organic Chemistry. 2002:3133-3139

Functionalised piperidines are frequently encountered structural motifs in bioactive compounds and in natural products.[1] The piperidine ring is often present as a substructure in drug-like molecules.[2] A well-known example is Ritalin (1, methyl α

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https://doi.org/10.1002/1099-0690(200209)2002:18<3133::aid-ejoc3133>3.0.co

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Development and application of allyl, 2-sulfonylethyl and 2-thioethyl carbamate linkers for solid phase N-acyliminium ion chemistry

Autor: Wim J. N. Meester, Henk Hiemstra, Floris P. J. T. Rutjes, Pedro H. H. Hermkens, Jan H. van Maarseveen, Chris G. Kruse, Johan J. N. Veerman

Publikováno v: Journal of the Chemical Society, Perkin Transactions 1. :994-1001

We have evaluated the allyl, 2-sulfonylethyl (SEC) and 2-thioethyl (TEC) carbamate linker systems for their application in solid supported N-acyliminium ion chemistry. As model reactions the syntheses of both homoallylic amines (via a three component

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https://doi.org/10.1039/b100998m

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A novel acid stable/base labile carbamate linker for N-acyliminium ion reactions on solid support

Autor: Henk Hiemstra, Jan H. van Maarseveen, Floris P. J. T. Rutjes, Johan J. N. Veerman

Publikováno v: Tetrahedron Letters. 40:6079-6082

The development of a novel carbamate linker optimized for solid phase N-acyliminium ion chemistry is reported. Some 2- and 2,4-substituted pyrrolidines were synthesized via addition of several carbon nucleophiles to immobilized N-acyliminium ions. A

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https://doi.org/10.1016/s0040-4039(99)01263-0

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Synthesis and use of water-soluble sulfonated dibenzofuran-based phosphine ligands

Autor: Piet W. N. M. van Leeuwen, Johan J. N. Veerman, Marcel Schreuder Goedheijt, Arjan E. Sollewijn Gelpke, Paul C. J. Kamer, Henk Hiemstra

Publikováno v: Tetrahedron. 55:6657-6670

The syntheses of three triphenylphosphine analogues with one, two or three phenyl groups replaced by 2-dibenzofuranyl groups, respectively, and one enantiopure analogue of the atropisomeric diphosphine MeO-BIPHEP with all four phenyl groups replaced

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https://doi.org/10.1016/s0040-4020(99)00312-9

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Synthesis of Enantiopure Functionalized Pipecolic Acids via Amino Acid DerivedN-Acyliminium Ions

Autor: Wim J. N. Meester, Hans E. Schoemaker, Henk Hiemstra, Johan J. N. Veerman, Floris P. J. T. Rutjes

Publikováno v: European Journal of Organic Chemistry. 1999:1127-1135

The synthesis and enzymatic resolution of a novel vinylsilane-containing amino acid is described. Derivatization of this and other olefinic amino acids followed by subjection to standard N-acyliminium ion cyclization conditions provides the correspon

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https://doi.org/10.1002/(sici)1099-0690(199905)1999:5<1127::aid-ejoc1127>3.0.co

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