A novel solid-phase synthesis of cyclic guanidines

We have developed a robust solid-phase approach to cyclic guanidines based on the Staudinger protocol. The synthetic sequence involves the reaction of the immobilized aza-Wittig reagents derived from the respective azidobenzoic acids with bifunctional amines. Convenient isolation and good yields of the desired products (34-84%) along with the diversity of the targeted molecules are distinctive features of the resultant library.