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Nucleophilic acyl substitution: the mechanism, step by step

The nucleophile adds to the carbonyl, the carbon holds four groups for a moment, and the leaving group is pushed out as the double bond comes back.

rule-derived3 stepsNot a record of what was observed

The pathway runs in 3 steps. What sits between them is a real structure: it is what the reaction passes through, and on a bad day it is what you isolate instead of the product.

Below is the sequence as it is taught. On the platform it is drawn on whatever structures you supply, with the curly arrows resolved to the actual atoms involved rather than to a general case with R groups on it.

The steps

  1. The nucleophile attacks the carbonyl carbon

    The nitrogen has a pair of electrons it is willing to share. It reaches the carbon of the C=O group, and the electrons of the double bond move onto the oxygen to make room.

    A lone pair on the nucleophile adds into the π* of the carbonyl. The carbon goes from three groups to four, the oxygen takes a negative charge and the nucleophile a positive one.

  2. The carbonyl comes back and the leaving group goes

    The oxygen pushes its electrons back down to remake the double bond, and that forces the chloride off the other side.

    The alkoxide collapses: the oxygen lone pair reforms the π bond and the C–leaving-group bond breaks heterolytically, the pair leaving with the departing atom.

  3. A base takes the proton

    The atom that attacked is still carrying a positive charge and a spare hydrogen. Something basic in the flask takes that hydrogen away, and the neutral product is left.

    Proton transfer from the cationic nucleophile to any base present — a second equivalent of the nucleophile, an added base, or the group that just left.

What this drawing assumes

Read these before you quote the mechanism
  • Addition and elimination are drawn as two steps. Whether the tetrahedral species is a true intermediate or only a transition state depends on the substrate, and for an acyl chloride it is short-lived.
  • Proton transfers are drawn as their own step and are fast compared with the two that make and break the bonds to carbon.

Other pathways this class runs by

  • A strongly acidic medium protonates the carbonyl oxygen first, which makes the carbon more electrophilic; the order of the middle two steps is then reversed.
  • With a poor leaving group and a strong nucleophile the addition can become rate-limiting rather than the collapse.

A class is not one pathway. Which of these runs depends on the substrate, the solvent and what else is in the flask, and the drawing above does not decide that for you.

Run it on your own structures

Enter the reactants and the product you expect. If the transformation is one the engine can perform and this pathway reaches that product from those structures, it is drawn on them — with the arrows on the right atoms and the intermediates you would actually pass through. If it does not reach the product, you are told that instead of being shown a drawing that does not apply.