A simple solid-phase synthesis of disubstituted guanidines using Rink amide resin as an amine component

A practical solid-phase synthesis that simply uses Rink amide resin as an amine component in reacting with aromatic isothiocyanates and aliphatic amines to generate disubstituted guanidines is described. No special linker or guanylation reagents are involved in this method. The product is obtained in a ‘traceless-linker’ fashion and in high yield and purity when an electron-deficient isothiocyanate is employed.