Solution and solid phase combinatorial synthesis of peptidomimetic library containing diversified alpha-methylated amino acids.

A combinatorial peptidomimetic library containing diversified alpha-methylated amino acids was generated by the Ugi four component condensation (4cc) reaction from acids, amines, isocyanides and ketones in both solution and solid phase synthetic procedures. This one-pot methodology overall gave fair to good yields, which compare well with multi-step syntheses.