Skeletal Diversity via a Branched Pathway: Efficient Synthesis of 29 400 Discrete, Polycyclic Compounds and Their Arraying into Stock Solutions

Abstract

We report the synthesis and arraying of 29 400 structurally diverse and complex polycyclic carbocycles using diversity-oriented synthesis (DOS) and the "one bead-one stock solution" technology platform. Skeletal diversity, a difficult challenge in DOS, was achieved with a branching reaction pathway using one or two Diels-Alder reactions. This pathway yields small molecules having 10 different skeletons.