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Manganese catalyst enables exploration of the magic methyl effect

The addition of a methyl group to a drug molecule can greatly alter the drug’s pharmacological properties. A catalyst has been developed that enables this ‘magic methyl effect’ to be rapidly explored for drug discovery.
  1. Emily B. Corcoran

    1. Emily B. Corcoran is in Process Research and Development, Merck & Co., Inc., Boston, Massachusetts 02115, USA.

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  2. Danielle M. Schultz

    1. Danielle M. Schultz is in Process Research and Development, Merck & Co., Inc., Kenilworth, New Jersey 07033, USA.

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Developing a small-molecule drug requires iterations of building and testing new compounds to find one that strikes the right balance of pharmacological properties. The process typically takes more than 10 years and costs billions of dollars, because, for every 5,000 compounds made and tested, only one will become an approved drug1,2. Indeed, a high-school basketball player is twice as likely to end up playing in the US professional league as any single compound tested in a drug-discovery programme is to become a marketed drug (see go.nature.com/2v8pnfm). One approach to accelerating drug discovery is late-stage functionalization, in which previously prepared test compounds are decorated with new atoms in the hope of favourably adjusting their pharmacological properties. Writing in Nature, Feng et al.3 report an outstanding advance towards this long-standing and historically challenging strategy.

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Nature 580, 592-593 (2020)

doi: https://doi.org/10.1038/d41586-020-01167-1

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