A strategy for the diversity-oriented synthesis of macrocyclic scaffolds using multidimensional coupling

Diversity oriented synthesis (DOS) aims to build structurally diverse compound libraries — potentially useful in drug discovery — from a small number of starting materials. Here, the build/couple/pair algorithm — commonly used in DOS — is extended to incorporate variations in the coupling step as well as in the starting materials. This produces a compound library with exceptionally high diversity in fewer than five steps from a common precursor.