The ‘magic’ methyl effect is a well-known chemistry idiom, describing the big effect that a single CH3 group can have on the bioactivity or selectivity of a molecule. However, it is currently tricky to simply stick a methyl onto an existing drug or natural product. Here, M. Christina White and colleagues report a Mn-catalysed oxidative C(sp3)–H methylation method that can install a methyl into various medicinally important heterocycles with high site-selectivity. This allows the modification of various natural products and drugs in a single step, providing the basis on which to better understand the ‘magic’ methyl effect and improve both current and new pharmaceutical agents.
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