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Midterm & Final Reference · Ultra-Dense A4
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CARBONYL CHEMISTRY — OVERVIEW ↗ TAP
The C=O electrophile

The carbonyl C is partially positive (δ+) — attacked by nucleophiles. The O is partially negative (δ−). Polarity drives nearly all carbonyl chemistry.

Reactivity ranking: acid chloride > anhydride > aldehyde > ketone > ester > carboxylic acid > amide
Carbonyl families
ClassR-CO-XX ispKa α-H
AldehydeR-CHOH~17
KetoneR-CO-R'R'~19
EsterR-COO-R'OR'~25
Carboxylic acidR-COOHOH (very acidic OH itself)~5 (OH); ~25 (α-H)
AmideR-CO-NR₂NR₂~30
Acid chlorideR-COClCl~16
Why ranking?
Better leaving groups (Cl⁻, RCOO⁻) speed reaction. Resonance donation from N or OR slows reaction (amide most stable, least reactive).
Aldehyde vs ketone
Aldehyde more reactive (less steric, less electron donation). Aldehydes oxidize easily to acids; ketones don't (no H to lose).

α-Carbon acidity: H next to C=O is acidic because the resulting enolate is resonance-stabilized. pKa ~ 19-20 for typical ketones.

⚡ EXAM TRAP — REACTIVITY ORDER ALWAYS STARTS WITH ACID CHLORIDE

Acid chloride > anhydride > aldehyde > ketone > ester > amide. Memorize. Used to predict who reacts first when multiple carbonyls are present, and to determine inter-conversion direction (always more → less reactive).

AMINES & AMIDES ↗ TAP
Amine basics

Lone pair on N makes amines basic and nucleophilic. Conjugate acid pKa ~ 10 (for RNH₃⁺). Aromatic amines (aniline, pKa 4.6) much weaker than aliphatic — N lone pair donates into ring.

ClassStructureExamples
R-NH₂methylamine
R₂NHdimethylamine
R₃Ntriethylamine
QuaternaryR₄N⁺permanently charged
Key reactions
Hofmann elimination
Quaternize amine with MeI excess → exhaustive methylation → Ag₂O / heat → least substituted alkene (Hofmann product).
Reductive amination
Aldehyde/ketone + amine → imine intermediate → reduce with NaBH₃CN or H₂/Pt → secondary or tertiary amine. Best route to make targeted amines.
Amide bond: RCOOH + R'NH₂ → RCONHR' (peptide bond)

Amides: resonance stabilization gives partial double bond character to C-N (planar, restricted rotation). Foundation of protein structure.

⚡ EXAM TRAP — ARYL AMINE BASICITY

Aniline (C₆H₅NH₂) is much weaker base than methylamine. The N lone pair conjugates into the ring, lowering availability for protonation. Adding electron-withdrawing groups to the ring (NO₂) further reduces basicity. Don't assume all amines have similar pKa.

NUCLEOPHILIC ADDITION (ALDEHYDES & KETONES) ↗ TAP
Mechanism — 2 steps

(1) Nu⁻ attacks carbonyl C from above or below the plane. (2) Proton (workup) gives alcohol.

R₂C=O + Nu⁻ → R₂C(O⁻)Nu →[H₂O] R₂C(OH)Nu
Nucleophiles + products
NucleophileProductNotes
NaBH₄, LiAlH₄1° or 2° alcoholNaBH₄ mild, LAH strong
RMgX (Grignard)alcohol, R addstetrahedral product
HCNcyanohydrinα-OH α-CN
H₂O / H⁺hydrate (gem-diol)usually unstable
R'OH / H⁺ (1 equiv)hemiacetalunstable
R'OH / H⁺ (2 equiv)acetalstable, protects carbonyl
RNH₂imine (R-N=R')via hemiaminal, lose H₂O
Acetal protection
Add 2 R'OH + acid + remove water → acetal. Stable to base, Grignard, hydride. Remove with aqueous acid to regenerate carbonyl.
Wittig reaction
RCHO + Ph₃P=CHR' → alkene R-CH=CHR' + Ph₃P=O. Best for converting C=O to C=C with control.

Reactivity: aldehydes > ketones (less steric, less electron donation). Aromatic carbonyls less reactive than aliphatic (resonance with ring).

⚡ EXAM TRAP — GRIGNARD + CARBONYL = ALCOHOL

Grignard (RMgX) attacks any carbonyl C. Don't forget: ester gives tertiary alcohol with TWO new R groups (Grignard adds twice — once to ester, once to ketone intermediate). Aldehyde gives 2° alcohol; ketone → 3° with one new R.

EAS — AROMATIC SUBSTITUTION ↗ TAP
Mechanism (2 steps)

(1) Electrophile E⁺ attacks ring → arenium ion (Wheland intermediate, loss of aromaticity). (2) Loss of H⁺ → restores aromaticity. Net: H replaced by E.

Ar-H + E⁺ → Ar-H-E⁺ → Ar-E + H⁺
5 main EAS reactions
RxnReagentProduct
HalogenationCl₂ or Br₂ + FeCl₃ / FeBr₃Ar-Cl, Ar-Br
NitrationHNO₃ + H₂SO₄Ar-NO₂
SulfonationSO₃ + H₂SO₄Ar-SO₃H (reversible)
F-C alkylationR-Cl + AlCl₃Ar-R (rearrangement risk!)
F-C acylationRCOCl + AlCl₃Ar-COR (no rearrangement)
Activator (ortho/para)
EDG (electron-donating): -OH, -NH₂, -OR, -R, halogens (weak deactivators but o/p-directing). Speed up rxn, direct to o/p.
Deactivator (meta)
EWG: -NO₂, -CN, -COR, -COOH, -SO₃H, -NR₃⁺. Slow rxn, direct meta. Halogens are exception (deactivate but o/p-directing).

F-C alkylation pitfalls: rearrangement of carbocation, polyalkylation (since alkyl is activator). Use F-C acylation then reduce to get straight-chain alkylated product.

⚡ EXAM TRAP — F-C FAILS ON DEACTIVATED RINGS

F-C alkylation and acylation don't work on rings with strong deactivators (NO₂, NR₃⁺) — the ring is too electron-poor. Plan multi-step syntheses to install the alkyl/acyl group before the deactivator.

NMR, IR & MASS SPEC ↗ TAP
¹H NMR — what each axis tells
FeatureTells you
chemical shift δ (ppm)chemical environment
# of signals# distinct H environments
integrationrelative # of H per signal
multiplicity (n+1)# neighboring H's
δ ranges: alkyl ~1 OH/NH ~2-5 broad aromatic 6-8 aldehyde 9-10 COOH 10-13
IR — diagnostic peaks
Carbonyls + alcohols
O-H broad 3200-3600. N-H sharp 3300. C=O strong sharp: acid chloride 1800, ester 1735, ketone 1715, amide 1680. O-H of acid (broad) 2500-3300.
Triple bonds + aromatic
C≡C / C≡N 2100-2260. Aromatic C=C 1600. Fingerprint < 1500: unique to compound.

Mass spec: M⁺ peak = molecular weight. Common fragments: M-15 (loss of CH₃), M-29 (CHO or C₂H₅), M-43 (C₃H₇ or COCH₃). Isotope patterns reveal Cl (M:M+2 = 3:1) and Br (1:1).

¹³C NMR: # of unique C environments. Ranges: alkyl 0-50, alkene 100-140, aromatic 120-140, carbonyl 170-220.

⚡ EXAM TRAP — n+1 RULE COUNTS NEIGHBORS, NOT SELF

For -CH₂-CH₃: the CH₂ sees 3 H's on CH₃ → quartet. The CH₃ sees 2 H's on CH₂ → triplet. You don't count your own H's. Off-by-one multiplicities lose questions reliably.

NUCLEOPHILIC ACYL SUBSTITUTION ↗ TAP
Mechanism — addition + elimination

Different from aldehyde/ketone addition: NAS proceeds via tetrahedral intermediate that kicks out a leaving group instead of just being protonated. Net: replaces LG with Nu.

R-CO-LG + Nu⁻ → [tetrahedral] → R-CO-Nu + LG⁻
Inter-conversions (always reactivity hierarchy)
FromToReagent
Acid chlorideanhydrideRCOO⁻
Acid chlorideesterR'OH (or NaOR')
Acid chlorideamideR'NH₂ (excess)
AnhydrideesterR'OH
AnhydrideamideR'NH₂
EsteramideR'NH₂ + heat
Esteracid (saponification)NaOH then H⁺
Fischer esterification
RCOOH + R'OH + H⁺ ⇌ RCOOR' + H₂O. Equilibrium — drive with excess R'OH or remove water.
Saponification
Ester + NaOH → carboxylate + alcohol. Irreversible (deprotonation of acid in basic conditions). Soap-making chemistry.

Carboxylic acid → ester: use Fischer (acid + alcohol) OR convert to acid chloride first then ROH (faster, irreversible).

⚡ EXAM TRAP — RUNS DOWNHILL ONLY

You can convert acid chloride to anything below it in reactivity. You can't go uphill directly (e.g. amide → ester). To go up the ladder, hydrolyze fully to acid, then re-derivatize. Plan synthesis routes accordingly.

ENOLATES & α-CHEMISTRY ↗ TAP
α-H is acidic
α-pKa ~20 (ketone, aldehyde) ~25 (ester) ~5 (1,3-dicarbonyls)

The α-H is between two electron-withdrawing groups (or next to one). Conjugate base (enolate) is resonance-stabilized — charge spreads onto O.

Reactions of enolates
RxnSetupProduct
Aldol2 carbonyls + base, mildβ-hydroxy carbonyl
Aldol condensationaldol + heat / strong baseα,β-unsaturated carbonyl (lose H₂O)
Claisen2 esters + NaOEtβ-keto ester
Michael additionenolate + α,β-unsat acceptor1,5-dicarbonyl
α-halogenationX₂ + acid OR baseα-haloketone
Aldol mechanism
(1) Base deprotonates α. (2) Enolate attacks carbonyl C of second molecule. (3) Workup gives β-hydroxy carbonyl. (4) Heat = aldol condensation.
Crossed aldol problem
2 different aldehydes/ketones with α-H → 4 products. Avoid by using a no-α-H partner (formaldehyde, benzaldehyde) or by directing enolate formation (LDA, kinetic).

1,3-Dicarbonyls (acetoacetate, malonate): pKa ~ 5-13. Strong enough to deprotonate with NaOEt. Used in syntheses (acetoacetic ester synthesis, malonic ester synthesis).

⚡ EXAM TRAP — KINETIC vs THERMODYNAMIC ENOLATE

For unsymmetric ketones: LDA (bulky, low T) deprotonates the less-substituted α (kinetic). NaOH/heat gives the more-substituted enolate (thermodynamic, more stable). Different conditions = different products.

DECISION BOX — PICK THE TECHNIQUE ↗ TAP
Match keyword to method
Question says…Use § fromApproach
'rank reactivity of carbonyls'§ ①acid chloride > anhydride > aldehyde > ketone > ester > amide
'aldehyde vs ketone'§ ②aldehyde more reactive; oxidizes to acid (Tollens, Jones)
'add Grignard to ester'§ ②2 equiv → 3° alcohol with two new R
'protect a carbonyl'§ ②form acetal with 2 R'OH/H⁺; remove with aq. acid
'C=C from C=O'§ ②Wittig (Ph₃P=CHR')
'convert acid to ester'§ ③Fischer (acid + alcohol + H⁺) OR via acid chloride
'saponify' / 'hydrolyze ester base'§ ③NaOH → carboxylate + alcohol (irreversible)
'acid chloride + amine'§ ③amide formation (use excess amine to absorb HCl)
'aldol condensation'§ ④base + 2 carbonyls → β-hydroxy → heat → α,β-unsat
'crossed aldol'§ ④use no-α-H partner OR LDA-controlled enolate
'Michael addition'§ ④enolate Nu + α,β-unsat C=O electrophile
'1,3-dicarbonyl synthesis'§ ④malonic / acetoacetic ester routes
'EAS, predict product'§ ⑤identify EDG/EWG, o/p vs meta director
'NO₂ before or after?'§ ⑤plan: Bromine first if you want o/p; nitrate first if you want meta
'F-C alkylation'§ ⑤watch rearrangement; use F-C acylation + reduce
'aniline basicity'§ ⑥much weaker than alkyl amine (lone pair into ring)
'reductive amination'§ ⑥aldehyde/ketone + amine + NaBH₃CN
'Hofmann elimination'§ ⑥quaternary ammonium → least subst alkene
NMR triplet 1.0 + quartet 4.0§ ⑦ethyl group next to electronegative atom
IR 1715 + 2.1 ppm singlet§ ⑦methyl ketone
IR broad 3000 + 1715 sharp§ ⑦carboxylic acid
Synthesis strategy
(1) ID functional groups in target. (2) Disconnect bonds at strategic positions (retrosynthesis). (3) Plan order — directors, protecting groups. (4) Choose mild reagents to avoid side reactions.
Mechanism arrows
From electron source (lone pair, π bond, anion) to electron sink (cation, electrophile). Each arrow = 2 e⁻. Don't break σ bonds for resonance.
⚡ EXAM TRAP — DRAW EVERY ARROW

Mechanisms earn partial credit per arrow. Skipping arrow notation = losing 50% even with right product. Source → sink, two electrons each.

⚡ FINAL EXAM TRAP — REARRANGEMENTS HAPPEN

Whenever a carbocation forms (SN1, E1, F-C alkylation, HX addition to alkenes), watch for 1,2-H or 1,2-alkyl shifts to a more stable C⁺. The 'expected' product may be wrong because the cation rearranged.

ORG CHEM II · Comprehensive Cram Sheet · Ultra-Dense A4
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