Improved and scalable synthesis of building blocks for the modular synthesis of teraryl-based alpha-helix mimetics

摘要

The modular synthesis of teraryl-based alphahelix mimetics can be accomplished by sequential Suzuki-couplings of arylboronic acid building blocks with 4-iodophenyltriflate core-fragments. We report about new synthetic accesses to core fragments featuring the side chains of Leu, Lys, Cys, Glu, Gln, Ser, and Thr starting from simple phenol precursors.