delta5-2-OXOPIPERAZINE DERIVATIVES AND SOLID-PHASE SYNTHESIS THEREOF

摘要

A synthesis method of Delta5-2-oxopiperazine derivatives by the cyclization of N-acyliminium-ion is provided to apply to a building block and synthesize the Delta5-2-oxopiperazine library member with high yield and purity. A solid phase synthesis method of Delta5-2-oxopiperazine derivatives of the chemical formula 1 comprises: a step of reacting bromoacetal resin with a first amine compound to obtain a second amine compound; a step of coupling the second amine compound with R2-substituted amino acid to obtain a compound (7); a step of removing a protection group by reacting the compound (7) with piperidine to obtain a compound (8); and a step of reacting the compound with formic acid to obtain a compound (9). The R3 compound has a R3 substitution group of acetyl, carbonyl, carbamate, nitro benzoate or amino group.