Halogenoalkanes – Learning Tool

🧪 Halogenoalkanes

📚 Extended Key Notes

Halogenoalkanes Definition & Classification

Definition: Compounds where one hydrogen atom in alkanes is replaced by a halogen atom (F, Cl, Br, I).

General Formula: R-X (alkyl halides), Ar-X (aryl halides)

Classification:

  • Primary (1°): Halogen attached to carbon bonded to only one other carbon
  • Secondary (2°): Halogen attached to carbon bonded to two other carbons
  • Tertiary (3°): Halogen attached to carbon bonded to three other carbons

Preparation of Halogenoarenes

Halogenation of Benzene:

Benzene + X₂ (Cl₂ or Br₂) + Fe or FeX₃ catalyst → Halogenobenzene

Mechanism: Electrophilic substitution

Catalyst Role: FeX₃ polarizes X-X bond, generating X⁺ electrophile

Example: C₆H₆ + Cl₂ → C₆H₅Cl + HCl

Reactivity Differences

Halogenoalkanes vs Halogenoarenes:

Chloroethane (R-Cl): Polar C-Cl bond, undergoes nucleophilic substitution

Chlorobenzene (Ar-Cl): Resonance stabilization, C-Cl bond has partial double bond character, undergoes electrophilic substitution

Reason: In chlorobenzene, lone pair on Cl delocalizes into benzene ring

Nucleophilic Substitution

General Reaction: R-X + Nu⁻ → R-Nu + X⁻

Key Components:

  • Substrate: Alkyl halide
  • Nucleophile: Electron-rich species (OH⁻, CN⁻, NH₃, etc.)
  • Leaving Group: Halogen ion (I⁻ > Br⁻ > Cl⁻ > F⁻)

SN1 vs SN2 Mechanisms

SN1 (Unimolecular):

  • Two-step mechanism
  • Forms carbocation intermediate
  • Favored by 3° alkyl halides
  • Racemic mixture product

SN2 (Bimolecular):

  • One-step mechanism
  • Backside attack
  • Favored by 1° alkyl halides
  • Inversion of configuration

Elimination Reactions

E1 (Unimolecular Elimination):

  • Two-step mechanism
  • Carbocation intermediate
  • Favored by 3° halides, weak bases

E2 (Bimolecular Elimination):

  • One-step mechanism
  • Concerted process
  • Favored by strong bases

🔍 Detailed Content

Preparation
Reactivity
SN Mechanisms
Elimination
Testing

Preparation of Halogenoarenes

Halogenoarenes (aryl halides) are prepared by electrophilic substitution of benzene with halogens in the presence of catalysts.

General Reaction: C₆H₆ + X₂ → C₆H₅X + HX

Catalysts: Fe, FeCl₃, FeBr₃, AlCl₃

Mechanism of Benzene Halogenation

  1. Generation of electrophile: Catalyst polarizes halogen molecule
  2. X₂ + FeX₃ → X⁺ + FeX₄⁻

  3. Electrophilic attack: X⁺ attacks benzene ring
  4. Formation of arenium ion: Stable intermediate
  5. Deprotonation: Regeneration of aromaticity

Example: Chlorination of Benzene

C₆H₆ + Cl₂ → C₆H₅Cl + HCl (in presence of FeCl₃)

Conditions: Room temperature, anhydrous conditions

Product: Chlorobenzene

Example: Bromination of Benzene

C₆H₆ + Br₂ → C₆H₅Br + HBr (in presence of FeBr₃)

Conditions: Room temperature, anhydrous conditions

Product: Bromobenzene

Important Notes

  • Fluorination is too vigorous and difficult to control
  • Iodination is reversible and requires oxidizing agents
  • Catalyst is essential for reaction to proceed at reasonable rate
  • Reaction follows electrophilic aromatic substitution mechanism

Reactivity of Halogenoalkanes vs Halogenoarenes

Chloroethane (Halogenoalkane)

Structure: CH₃-CH₂-Cl

Bond Character: Polar covalent bond

Electron Distribution: Carbon δ⁺, Chlorine δ⁻

Reactivity: High towards nucleophiles

Reaction Type: Nucleophilic substitution

CH₃-CH₂-Cl + OH⁻ → CH₃-CH₂-OH + Cl⁻

Chlorobenzene (Halogenoarene)

Structure: C₆H₅-Cl

Bond Character: Partial double bond due to resonance

Electron Distribution: Delocalized in ring

Reactivity: Low towards nucleophiles

Reaction Type: Electrophilic substitution

C₆H₅-Cl + NO₂⁺ → o-NO₂-C₆H₄-Cl + p-NO₂-C₆H₄-Cl

Resonance in Chlorobenzene

The C-Cl bond in chlorobenzene has partial double bond character due to resonance:

Cl donates lone pair to benzene ring → C-Cl bond gains double bond character

This makes the bond shorter and stronger than in alkyl chlorides

Factors Affecting Reactivity

  • Bond Strength: C-Cl bond stronger in aryl halides due to resonance
  • Steric Effects: Bulky benzene ring hinders nucleophilic attack
  • Electronic Effects: Electron-rich benzene ring repels nucleophiles
  • Hybridization: sp² hybridized carbon in aryl halides vs sp³ in alkyl halides

Nucleophilic Substitution Mechanisms

SN1 Mechanism (Unimolecular)

Steps:

  1. Slow step: Ionization to form carbocation
  2. R-X → R⁺ + X⁻ (rate-determining)

  3. Fast step: Nucleophile attack
  4. R⁺ + Nu⁻ → R-Nu

Rate Law: Rate = k[R-X]

Favored by: 3° alkyl halides, polar protic solvents, weak nucleophiles

Stereochemistry: Racemic mixture (both enantiomers)

SN2 Mechanism (Bimolecular)

Steps:

  1. Concerted process: Single step
  2. Nu⁻ + R-X → [Nu—R—X]⁻ → R-Nu + X⁻

Rate Law: Rate = k[Nu⁻][R-X]

Favored by: 1° alkyl halides, polar aprotic solvents, strong nucleophiles

Stereochemistry: Inversion of configuration (backside attack)

Carbocation Stability

The stability order of carbocations determines SN1 reaction rates:

Stability Order: 3° > 2° > 1° > methyl

Reason: Hyperconjugation and inductive effects from alkyl groups

Alkyl Halide Type Preferred Mechanism Reason
Primary (1°) SN2 Less steric hindrance, unstable carbocation
Secondary (2°) Both SN1 and SN2 Moderate steric hindrance, moderately stable carbocation
Tertiary (3°) SN1 High steric hindrance, stable carbocation

Solvent Effects

  • Polar Protic Solvents (water, alcohols): Favor SN1 by stabilizing carbocation and leaving group
  • Polar Aprotic Solvents (acetone, DMSO): Favor SN2 by activating nucleophile

Elimination Reactions

E1 Mechanism (Unimolecular Elimination)

Steps:

  1. Ionization: Formation of carbocation
  2. R-X → R⁺ + X⁻

  3. Deprotonation: Base removes β-hydrogen
  4. R⁺ + B⁻ → Alkene + H-B

Rate Law: Rate = k[R-X]

Favored by: 3° alkyl halides, weak bases, polar protic solvents

Regioselectivity: Follows Zaitsev’s rule (more substituted alkene)

E2 Mechanism (Bimolecular Elimination)

Steps:

  1. Concerted process: Single step
  2. B⁻ + R-X → Alkene + H-B + X⁻

Rate Law: Rate = k[B⁻][R-X]

Favored by: Strong bases, polar aprotic solvents

Stereochemistry: Anti-periplanar arrangement required

Competition Between Substitution and Elimination

Alkyl Halide Strong Base/Nucleophile Weak Base/Nucleophile
Primary (1°) SN2 (major), E2 (minor) SN2
Secondary (2°) E2 (major), SN2 (minor) SN1/E1 mixture
Tertiary (3°) E2 E1/SN1 mixture

Testing Halogenoalkane Reactivity

Silver Nitrate Test

A common test to assess halogenoalkane reactivity uses aqueous silver nitrate (AgNO₃).

General Reaction: R-X + AgNO₃ → R-ONO₂ + AgX↓

Reactivity Order

The reactivity follows the order: RI > RBr > RCl > RF

Reason: Decreasing C-X bond strength down the group

Halogenoalkane Precipitate Color Solubility in NH₄OH Reactivity
R-F No precipitate Very low
R-Cl White Soluble Low
R-Br Cream Partially soluble Medium
R-I Yellow Insoluble High

Bond Strength Explanation

  • C-F bond: Strongest due to small size and high electronegativity of F
  • C-I bond: Weakest due to large size and poor orbital overlap
  • Trend: Bond strength decreases down the group: C-F > C-Cl > C-Br > C-I

💡 Tips, Tricks & Memorization Techniques

🧠 SN1 vs SN2 Mnemonic

“1-2-3 Rule”:

alkyl halides → SN2

alkyl halides → SN1

alkyl halides → Can do both

🔢 Carbocation Stability

“The More, The Merrier”:

More alkyl groups = More stable carbocation

Order: 3° > 2° > 1° > CH₃⁺

Reason: Hyperconjugation and inductive effects

🔄 Reactivity Order Memory Aid

Silver Nitrate Test:

RI > RBr > RCl > RF

Mnemonic: “I Bring Cool Friends”

Remember: Bond strength decreases down the group

⚖️ Solvent Effects

Protic vs Aprotic:

Protic (H-bond donors): Favor SN1/E1

Aprotic (no H-bond donors): Favor SN2/E2

Examples: Water/alcohols (protic) vs Acetone/DMSO (aprotic)

🎯 Leaving Group Ability

Good Leaving Groups: I⁻, Br⁻, Cl⁻, HSO₄⁻

Poor Leaving Groups: OH⁻, OR⁻, NH₂⁻

Rule: Weak bases make good leaving groups

🔍 Halogenoarene vs Halogenoalkane

Halogenoalkane: C-X bond polar, nucleophilic substitution

Halogenoarene: C-X bond partial double bond, electrophilic substitution

Memory: “Arenes like Electrophiles, Alkanes like Nucleophiles”

📝 Exercise Solutions

Multiple Choice Questions

i. Which catalyst is commonly used in the halogenation of benzene with Cl₂ or Br₂?

a) H₂SO₄
b) FeCl₃
c) AlCl₃
d) NaOH

Answer: b) FeCl₃

Explanation: FeCl₃ or FeBr₃ are commonly used as Lewis acid catalysts in the halogenation of benzene. They polarize the halogen molecule, generating the electrophile needed for the reaction.

ii. In the reaction of benzene with Cl₂ in the presence of a catalyst, the product is:

a) Chloromethane
b) Chlorobenzene
c) Dichloromethane
d) Benzyl chloride

Answer: b) Chlorobenzene

Explanation: Benzene undergoes electrophilic substitution with chlorine in the presence of FeCl₃ catalyst to form chlorobenzene (C₆H₅Cl).

iii. What is the major product of the reaction between benzene and Br₂ with FeBr₃ as a catalyst?

a) Benzene bromide
b) Bromobenzene
c) Dibromobenzene
d) Bromomethane

Answer: b) Bromobenzene

Explanation: The reaction produces bromobenzene (C₆H₅Br) through electrophilic aromatic substitution. Further bromination requires more vigorous conditions.

iv. Which mechanism do primary halogenoalkanes typically follow in nucleophilic substitution reactions?

a) SN1
b) SN2
c) SN1 and SN2 both
d) None of these

Answer: b) SN2

Explanation: Primary halogenoalkanes prefer SN2 mechanism due to less steric hindrance and the instability of primary carbocations for SN1.

v. What type of bond is broken in the nucleophilic substitution reaction of a halogenoalkane?

a) C-H
b) C-O
c) C-X (where X is a halogen)
d) C-C

Answer: c) C-X (where X is a halogen)

Explanation: In nucleophilic substitution reactions, the carbon-halogen bond (C-X) is broken as the halogen is replaced by a nucleophile.

vi. Which factor does NOT significantly affect the rate of SN1 reactions?

a) Stability of the carbocation
b) Solvent polarity
c) Strength of the nucleophile
d) Leaving group ability

Answer: c) Strength of the nucleophile

Explanation: SN1 reactions are unimolecular and the rate depends only on the concentration of the substrate. The nucleophile concentration doesn’t affect the rate since it attacks in the fast second step.

vii. Which halogenoalkane is more reactive in an SN2 reaction?

a) Chloromethane
b) Chlorobenzene
c) Chloroethane
d) All of these

Answer: a) Chloromethane

Explanation: Chloromethane (CH₃Cl) is the most reactive in SN2 reactions because it has the least steric hindrance around the carbon bearing the chlorine.

viii. The C-Cl bond in chlorobenzene is less reactive towards nucleophilic substitution because:

a) The C-Cl bond is too strong
b) The phenyl ring stabilizes the chlorine
c) Resonance effect makes the bond partially double
d) Steric hindrance from the benzene ring

Answer: c) Resonance effect makes the bond partially double

Explanation: In chlorobenzene, the lone pair on chlorine delocalizes into the benzene ring through resonance, giving the C-Cl bond partial double bond character, making it stronger and less reactive.

ix. When chloroethane reacts with aqueous silver nitrate, the precipitate formed is:

a) Silver chloride
b) Silver nitrate
c) Silver oxide
d) No precipitate forms

Answer: a) Silver chloride

Explanation: Chloroethane reacts slowly with silver nitrate to form silver chloride (AgCl) precipitate, which is white and soluble in ammonia.

Short Answer Questions

i. Describe the halogenation of benzene.

Answer: Halogenation of benzene involves the electrophilic substitution of a hydrogen atom by a halogen atom (Cl or Br) in the presence of a Lewis acid catalyst like FeCl₃ or FeBr₃.

Mechanism:

  1. The catalyst polarizes the halogen molecule: X₂ + FeX₃ → X⁺ + FeX₄⁻
  2. The electrophile (X⁺) attacks the benzene ring, forming an arenium ion intermediate
  3. The arenium ion loses a proton to regenerate the aromatic system

Example: C₆H₆ + Cl₂ → C₆H₅Cl + HCl (with FeCl₃ catalyst)

ii. Explain why chlorobenzene is less reactive than chloroethane in nucleophilic substitution reactions.

Answer: Chlorobenzene is less reactive than chloroethane in nucleophilic substitution due to:

  1. Resonance stabilization: The lone pair on chlorine delocalizes into the benzene ring, giving the C-Cl bond partial double bond character
  2. Stronger C-Cl bond: The resonance makes the bond shorter and stronger than in alkyl chlorides
  3. sp² hybridization: The carbon in chlorobenzene is sp² hybridized, making it less accessible to nucleophiles
  4. Electronic effects: The electron-rich benzene ring repels nucleophiles

In contrast, chloroethane has a polar C-Cl bond with no resonance stabilization, making it more susceptible to nucleophilic attack.

iii. What is the major product when benzene reacts with Br₂ in the presence of FeBr₃?

Answer: The major product is bromobenzene (C₆H₅Br).

Reaction: C₆H₆ + Br₂ → C₆H₅Br + HBr (with FeBr₃ catalyst)

Mechanism: Electrophilic aromatic substitution where Br⁺ attacks the benzene ring.

Note: Further bromination to form dibromobenzene requires more vigorous conditions as the first bromine deactivates the ring towards further electrophilic substitution.

Long Answer Questions

i. Explain the mechanisms of SN1 and SN2 reactions in detail, including the factors that affect each mechanism and examples of substrates that prefer each pathway.

Answer:

SN1 Mechanism (Unimolecular Nucleophilic Substitution)

Steps:

  1. Slow ionization: R-X → R⁺ + X⁻ (rate-determining step)
  2. Fast nucleophilic attack: R⁺ + Nu⁻ → R-Nu

Rate Law: Rate = k[R-X] (first order)

Stereochemistry: Racemic mixture (both enantiomers formed equally)

SN2 Mechanism (Bimolecular Nucleophilic Substitution)

Steps:

  1. Concerted process: Nu⁻ + R-X → [Nu—R—X]⁻ → R-Nu + X⁻ (single step)

Rate Law: Rate = k[Nu⁻][R-X] (second order)

Stereochemistry: Inversion of configuration (backside attack)

Factors Affecting Mechanism Preference

1. Structure of Alkyl Halide:

  • Primary (1°): Prefer SN2 (less steric hindrance)
  • Tertiary (3°): Prefer SN1 (stable carbocation, high steric hindrance)
  • Secondary (2°): Can undergo both mechanisms

2. Nature of Nucleophile:

  • Strong nucleophiles: Favor SN2 (OH⁻, CN⁻, I⁻)
  • Weak nucleophiles: Favor SN1 (H₂O, ROH)

3. Solvent Effects:

  • Polar protic solvents: Favor SN1 (stabilize ions)
  • Polar aprotic solvents: Favor SN2 (activate nucleophile)

4. Leaving Group Ability:

  • Better leaving groups favor both mechanisms: I⁻ > Br⁻ > Cl⁻ > F⁻

Examples

SN2 Preferred: CH₃-Br + OH⁻ → CH₃-OH + Br⁻ (methyl bromide)

SN1 Preferred: (CH₃)₃C-Br + H₂O → (CH₃)₃C-OH + H⁺ + Br⁻ (tert-butyl bromide)

ii. Compare and contrast the reactivity of halogenoalkanes and halogenoarenes with examples. Discuss the factors contributing to their differing reactivities.

Answer:

Aspect Halogenoalkanes (e.g., Chloroethane) Halogenoarenes (e.g., Chlorobenzene)
General Formula R-X Ar-X
Bond Character Polar covalent bond Partial double bond due to resonance
Reactivity towards Nucleophiles High Very low
Reactivity towards Electrophiles Low High (ring substitution)
Preferred Reaction Type Nucleophilic substitution Electrophilic substitution
Bond Strength (C-X) Weaker Stronger
Hybridization of Carbon sp³ sp²

Factors Contributing to Different Reactivities

1. Resonance Effect:

  • Halogenoarenes: Lone pair on halogen delocalizes into benzene ring, creating partial double bond character
  • Halogenoalkanes: No resonance stabilization, pure single bond

2. Bond Strength:

  • Halogenoarenes: C-X bond shorter and stronger (~169 pm, ~400 kJ/mol for C-Cl)
  • Halogenoalkanes: C-X bond longer and weaker (~177 pm, ~340 kJ/mol for C-Cl)

3. Electronic Effects:

  • Halogenoarenes: Halogen is ortho-para director but deactivates ring towards electrophiles
  • Halogenoalkanes: Halogen withdraws electrons inductively, making carbon electrophilic

4. Steric Effects:

  • Halogenoarenes: Flat structure allows resonance but hinders nucleophilic approach
  • Halogenoalkanes: Tetrahedral structure more accessible to nucleophiles

Examples of Reactions

Chloroethane: CH₃-CH₂-Cl + OH⁻ → CH₃-CH₂-OH + Cl⁻ (nucleophilic substitution)

Chlorobenzene: C₆H₅-Cl + HNO₃ → o-NO₂-C₆H₄-Cl + p-NO₂-C₆H₄-Cl (electrophilic substitution)