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Rapid synthesis a thousand times

Nature volume 515, page 468 (27 November 2014) | Download Citation


A robotic system that can carry out and analyse 1,536 chemical reactions in less than a day could help to accelerate drug discovery.

Tim Cernak and Spencer Dreher at pharmaceutical company Merck in Massachusetts and New Jersey and their colleagues used the system to couple a model substrate with 16 other molecules, in combination with 16 different palladium catalysts and 6 basic reagents. Each of these unique mixtures was dissolved in 1 microlitre of solvent, automatically dispensed into a separate chamber on a 1,536-well plate, and its products were analysed to determine optimum reaction conditions.

The researchers also coupled pairs of more-complex, drug-like substrates, and easily scaled up successful reactions by 1,000 times or more. This high-throughput approach could rapidly assess synthetic routes to a wide range of drug candidates without wasting precious starting materials.

Science (2014)

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