134172-65-9Relevant articles and documents
Structure-Based Design of High-Affinity Fluorescent Probes for the Neuropeptide Y Y1Receptor
Müller, Christoph,Gleixner, Jakob,Tahk, Maris-Johanna,Kopanchuk, Sergei,Laasfeld, T?nis,Weinhart, Michael,Schollmeyer, Dieter,Betschart, Martin U.,Lüdeke, Steffen,Koch, Pierre,Rinken, Ago,Keller, Max
, p. 4832 - 4853 (2022/03/27)
The recent crystallization of the neuropeptide Y Y1 receptor (Y1R) in complex with the argininamide-type Y1R selective antagonist UR-MK299 (2) opened up a new approach toward structure-based design of nonpeptidic Y1R ligands. We designed novel fluorescent probes showing excellent Y1R selectivity and, in contrast to previously described fluorescent Y1R ligands, considerably higher (～100-fold) binding affinity. This was achieved through the attachment of different fluorescent dyes to the diphenylacetyl moiety in 2 via an amine-functionalized linker. The fluorescent ligands exhibited picomolar Y1R binding affinities (pKi values of 9.36-9.95) and proved to be Y1R antagonists, as validated in a Fura-2 calcium assay. The versatile applicability of the probes as tool compounds was demonstrated by flow cytometry- and fluorescence anisotropy-based Y1R binding studies (saturation and competition binding and association and dissociation kinetics) as well as by widefield and total internal reflection fluorescence (TIRF) microscopy of live tumor cells, revealing that fluorescence was mainly localized at the plasma membrane.
CoI-Catalyzed Barbier Reactions of Aromatic Halides with Aromatic Aldehydes and Imines
Presset, Marc,Paul, Jér?me,Cherif, Ghania Nait,Ratnam, Nisanthan,Laloi, Nicolas,Léonel, Eric,Gosmini, Corinne,Le Gall, Erwan
supporting information, p. 4491 - 4495 (2019/02/27)
The reductive Barbier coupling of aromatic halides and electrophiles has been achieved using a CoBr2/1,10-phenanthroline catalytic system and over stoichiometric amounts of zinc. The reaction displayed a broad scope of substrates, including (hetero)aryl chlorides as pro-nucleophiles and aldehydes or imines as electrophiles, leading to diarylmethanols and diarylmethylamines in moderate to excellent yields, respectively.
Synthesis method for diaryl methanol compound
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Paragraph 0074; 0075; 0076; 0077; 0102; 0103-0123, (2018/03/26)
The technical solution and content of the invention relate to a synthesis method for a diaryl methanol compound shown as formula (I); the formula (I) is shown in the specification. The method includesthe following steps: under the existence of a palladium-sourced compound catalyst and organic phosphine ligand, in an organic solvent, an aldehyde derivative shown as formula (II) reacts with an organic cyclic triolborate compound shown as formula (III), and after the reaction is completed, post-processing is carried out, so that the diaryl methanol compound shown as formula (I) is obtained. According to the method, the reaction between the aldehyde compound and the organic cyclic triolborate compound can be smoothly carried out, so that the diaryl methanol compound can be obtained at high yield, a brand new synthesis route is provided for the synthesis of the compound, and a good application prospect and good industrial value are achieved.
