900800-02-4Relevant articles and documents
AMINO-ACID ANILIDES AS SMALL MOLECULE MODULATORS OF IL-17
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Page/Page column 71-72, (2020/07/14)
The present invention relates to a compound according to formula I (I) and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention further relates to said compounds for use in therapy, to pharmaceutical compositions comprising said compounds, to methods of treating diseases, e.g. dermal diseases, with said compounds, and to the use of said compounds in the manufacture of medicaments.
Enhanced copper-mediated 18F-fluorination of aryl boronic esters provides eight radiotracers for PET applications
Preshlock, Sean,Calderwood, Samuel,Verhoog, Stefan,Tredwell, Matthew,Huiban, Mickael,Hienzsch, Antje,Gruber, Stefan,Wilson, Thomas C.,Taylor, Nicholas J.,Cailly, Thomas,Schedler, Michael,Collier, Thomas Lee,Passchier, Jan,Smits, René,Mollitor, Jan,Hoepping, Alexander,Mueller, Marco,Genicot, Christophe,Mercier, Jo?l,Gouverneur, Véronique
supporting information, p. 8361 - 8364 (2016/07/07)
[18F]FMTEB, [18F]FPEB, [18F]flumazenil, [18F]DAA1106, [18F]MFBG, [18F]FDOPA, [18F]FMT and [18F]FDA are prepared from the corresponding arylboronic esters and [18
Evidence for the role of tetramethylethylenediamine in aqueous negishi cross-coupling: Synthesis of nonproteinogenic phenylalanine derivatives on water
Ross, Andrew J.,Dreiocker, Frank,Schae Fer, Mathias,Oomens, Jos,Meijer, Anthony J.H.M.,Pickup, Barry T.,Jackson, Richard F.W.
supporting information; experimental part, p. 1727 - 1734 (2011/05/30)
The structure of the alkylzinc-tetramethylethylenediamine (TMEDA) cluster cation 3 has been determined in the gas phase by a combination of tandem mass spectrometry, infrared multiphoton dissociation (IRMPD) spectroscopy, and DFT calculations. Both sets of experimental results establish the existence of a strongly stabilizing interaction of TMEDA with the zinc cation. High-level DFT calculations on the alkylzinc-TMEDA cluster cation 3 allowed the identification of two low energy conformers, each featuring a four-coordinate zinc atom with a bidentate TMEDA ligand, and internal coordination from the carbonyl group of the Boc group to zinc. The experimental IRMPD spectrum is reproduced with an appropriately weighted combination of the IR spectra of the two conformers identified by theory. DFT calculations on the structure of the alkylzinc halide 2 with coordinated TMEDA using the PCM model of water solvent suggest that TMEDA can promote ionization of the zinc-iodine bond in organozinc iodides under aqueous conditions, providing a credible explanation for the role of TMEDA in stabilizing the carbon-zinc bond. Reaction of the serine-derived iodide 1 with aryl iodides "on water", promoted by nano zinc in the presence of PdCl2 (Amphos) 2 (5 mol %) and TMEDA, leads to the formation of protected phenylalanine derivatives 4 in reasonable yields. In the case of ortho-substituted aryl iodides and aryl iodides that are solids at room temperature, conducting the reaction at 65°C gives improved results. In all cases, the product 5 of reductive dimerization of the iodide 1 is also isolated.