High-throughput experimentation (HTE) chemistry is rarely used in the area where it may have the most benefit: towards the preparation of complex organic molecules. In this presentation, the idea is explored, using palladium-catalyzed cross-coupling reactions on complex drug-like molecules as the test case, that synthetic methods from the chemistry literature can be evolved into a powerful substrate-sparing chemistry platform for problem-solving that can be executed on standard biochemical nano-liter robots in plastic 1536 well-plates. This nanomolar scale approach leads to conditions that are highly scalable for useful preparative quantities. Application of modern high-throughput mass-spectrometric methods allows for same-day analysis of 1536 complex reactions.

Nanomolar scale high throughput chemistry for complex molecules synthesis

249th National Meeting (2015)

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