A NOVEL CLEAVAGE TECHNIQUE TO GENERATE SMALL-MOLECULE COMPOUNDS AND LIBRARIES VIA A 2-RESIN SYSTEM

Application of organic synthesis to solid supports has led to the succ essful implementation of combinatorial chemistry in the drug discovery process. This paper describes a novel use of the Hofmann elimination of tetrasubstituted amine salts on solid-phase resin to generate diver se combinatorial libraries of trisubstituted amines. Highly pure compo unds were isolated without further purification by the addition of a s econd resin as the source reagent to promote the required elimination. The use of mixed resin systems to generate compounds is a novel appli cation of bead-based technologies.