从炼金术到精准骨架编辑

Atoms are selectively replaced, added, or deleted within ring-shaped molecules Jimmy Wu M edieval alchemists dreamt of transmuting base metals, such as lead, into gold. Similarly, modern organic chemists dream of transforming one atom of a molecule into another atom without disturbing the original structure. Selectively converting a carbon atom of a carbocycle—a ring-shaped molecule containing only carbon—into a nitrogen atom results in the formation of a nitrogen heterocycle, which comprise more than 59% of small-molecule drugs approved by the US Food and Drug Administration (1). However, swapping a carbon atom with another atom is an extremely difficult task because this requires breaking strong C–C bonds. On pages 528 and 536 of this issue, Li et al. …