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What is the significance of leaving groups in nucleophilic aromatic substitution?

Here’s the explanation of the role of leaving groups in nucleophilic aromatic substitution (SNAr):


1. Quality of Leaving Group

  • A good leaving group makes it easier for the nucleophile to replace it.
  • Typical leaving groups: F > Cl > Br > I (unusual order compared to aliphatic substitution).

2. Why is Fluorine the Best Here?

  • In SNAr, the key step is nucleophilic attack forming the Meisenheimer complex.
  • Fluorine strongly withdraws electrons (highly electronegative), making the ring carbon more positive and easier to attack.
  • That’s why Ar–F reacts fastest, even though F⁻ is usually a poor leaving group in other reactions.

3. Position Relative to Electron-Withdrawing Groups

  • Leaving group must be ortho or para to strong EWGs (like –NO₂).
  • This allows the negative charge in the intermediate to be stabilized, helping the leaving group go away.

In short:

  • The leaving group controls how easily substitution happens.
  • In SNAr: F > Cl > Br > I because fluorine activates the ring the most.
  • Leaving group must be near EWGs to make the reaction fast.

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