Industrial natural product chemistry for drug discovery and development

Covering: up to March 2013 In addition to their prominent role in basic biological and chemical research, natural products are a rich source of commercial products for the pharmaceutical and other industries. Industrial natural product chemistry is of fundamental importance for successful product development, as the vast majority ( ca. 80%) of commercial drugs derived from natural products require synthetic efforts, either to enable economical access to bulk material, and/or to optimize drug properties through structural modifications. This review aims to illustrate issues on the pathway from lead to product, and how they have been successfully addressed by modern natural product chemistry. It is focused on natural products of current relevance that are, or are intended to be, used as pharmaceuticals. Twelve case studies illustrate common issues on the avenue from a natural product-based lead compound to a pharmaceutical drug product, and how they have been successfully addressed by modern synthetic methods.