4-N-ACYL- DELTA 5-2-OXOPIPERAZINES, A PROCESS FOR ITS PREPARATION AND COMBINATORIAL LIBRARIES THEREOF

摘要

A novel solution phase and solid phase synthesis of 4-N-acyl- DELTA 5-2-oxopiperazine (I) is described via a Ugi four-component condensation of an acid, an ketone or aldehyde, a protected alpha -aminoaldehyde or alpha -aminoketone and an isocyanide followed by an N-acyliminium ion cyclization facilitated by an acid, which also cleaves the product from the polymer when the reaction is conducted in the solid phase.