Combinatorial solid-phase natural product chemistry

Abstract

One major challenge in combinatorial chemistry is to find biologically relevant starting points in the chemical universe around which compound libraries should be produced. Natural products represent such biologically validated starting points. Progress in Solid-Phase Organic Synthesis (SPOS) has enabled now the combination of natural product synthesis with combinatorial methods. Two strategies can be distinguished:(1) Attachment of a natural product core structure onto solid phase and subsequent modification of functional groups, or (2) total synthesis of the complete natural product scaffold on solid phase. A complementary approach identifies privileged structures among natural product scaffolds, which serve as inspiration for library synthesis. In this review the current status and the challenges of combinatorial natural product synthesis on solid phase are presented. . © Springer-Verlag Berlin Heidelberg.