Trobe, Melanie; Vareka, Martin; Schreiner, Till; Dobrounig, Patrick; Doler, Carina; Holzinger, Ella B.; Steinegger, Andreas; Breinbauer, Rolf published the artcile< A Modular synthesis of teraryl-based α-helix mimetics, part 3: Iodophenyltriflate core fragments featuring side chains of proteinogenic amino acids>, Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine, the main research area is peptidomimetic helix teraryl amino acid synthesis protein interaction inhibitor; Suzuki Miyaura coupling Wittig reaction iodo salicylic aldehyde amination; Inhibitors; Peptide mimetics; Protein–protein interactions; Suzuki coupling; Triflate.
Teraryl-based α-helix mimetics have proven to be useful compounds for the inhibition of protein-protein interactions (PPI). We have developed a modular and flexible approach for the synthesis of teraryl-based α-helix mimetics using a benzene core unit featuring two leaving groups of differentiated reactivity in the Pd-catalyzed cross-coupling used for teraryl assembly. In previous publications we have introduced the methodol. of 4-iodophenyltriflates decorated with the side chains of some of the proteinogenic amino acids. We herein report the core fragments corresponding to the previously missing amino acids Arg, Asn, Asp, Met, Trp and Tyr. Therefore, our set now encompasses all relevant amino acid analogs with the exception of His. In order to be compatible with the triflate moiety, some of the nucleophilic side chains had to be provided in a protected form to serve as stable building blocks. Addnl., cross-coupling procedures for the assembly of teraryls were investigated.
European Journal of Organic Chemistry published new progress about Amination. 329214-79-1 belongs to class pyridine-derivatives, and the molecular formula is C11H16BNO2, Recommanded Product: 3-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine.