October 20, 2003

Constrained Peptidomimetics: Building Bicyclic Analogs of Pyrazoline Derivatives

Bin Liu, John D Brandt and Kevin D Moeller
Tetrahedron, 2003, 59 (43), 8515-8523

A synthetic route has been developed for incorporating pyrazoline derivatives as proline surrogates in constrained X-Pro peptidomimetics. The route allows for the synthesis of dipeptide building blocks having either a six or seven-membered-ring annulated onto the pyrazoline moiety, as well as for the asymmetric synthesis of analogs having substituents on N-terminal side of the building block.