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Metalation introduces a metal into a molecule or replaces an attached atom or group with a metal-containing connection. In organometallic chemistry, the term often refers to forming a carbon–metal chemical bond, for example by replacing a carbon-bound hydrogen.

The word describes the transformation, while the mechanism can involve proton transfer, metal insertion or other pathways. A metalated carbon centre may act as a nucleophile in a subsequent bond-forming reaction. Which site is metalated depends on acidity, coordination and kinetics, so the most acidic isolated bond need not uniquely predict the product under every reaction condition.