Template Synthesis of Peptidomimetics Composed of Aspartic Acid Moiety by Ugi Four‐Component Condensation Reaction

Caspase‐3 inhibitors were supposed to be of benefit to both acute and chronic neurodegenerative conditions. In this work, a CPP32‐peptidomimetic‐inhibitor library was designed. The necessary aspartate moiety was reserved at the C terminal. A facile and versatile method based on Ugi‐4CR was developed to build up the library. The aspartic acid–derived isocyanide 3, the most important component of the four, was effectively synthesized from protected aspartic acid. This Ugi procedure was tested by synthesizing a small library.