Abstract: Aim To find a reasonable way to prepare the designed CPP32 inhibitors. Method Ugi four-component condensation reaction was used to synthesize peptide mimic CPP32 inhibitors; Results A key isocyanide component (aspartate-derived isocyanide 3) and one of the designed CPP32 inhibitors 4 (as a template) were synthesized; Conclusion The CPP32 inhibitor 4 was synthesized by the newly developed procedure, which is an Ugi four-component condensation reaction based on aspartate-derived isocyanide 3. This method can be used to build up the CPP32 inhibitor library.

Key words: CPP32, CPP32, Ugi-4CR, Ugi-4CR, isocyanide, isocyanide