Ketones as strategic building blocks for the synthesis of natural product-inspired compounds

Natural product-inspired compound collections serve as excellent sources for the identification of new bioactive compounds to treat disease. However, such compounds must necessarily be more structurally-enriched than traditional screening compounds, therefore inventive synthetic strategies and reliable methods are needed to prepare them. Amongst the various possible starting materials that could be considered for the synthesis of natural product-inspired compounds, ketones can be especially valuable due to the vast variety of complexity-building synthetic transformations that they can take part in, their high prevalence as commercial building blocks, and relative ease of synthesis. With a view towards developing a unified synthetic strategy for the preparation of next generation bioactive compound collections, this review considers whether ketones could serve as general precursors in this regard, and summarises the opulence of synthetic transformations available for the annulation of natural product ring-systems to ketone starting materials.

Automated summary

Natural product-inspired compound collections are important sources for discovering new bioactive compounds for treating diseases. Ketones, with their variety of synthetic transformations, prevalence as commercial building blocks, and relative ease of synthesis, can be valuable as starting materials for the synthesis of natural product-inspired compounds. This review explores the use of ketones as general precursors and summarizes the synthetic transformations available for the annulation of natural product ring-systems to ketone starting materials.