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Carboxylic Acids

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Carboxylic Acids
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12/2/2011
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Carboxylic acids:

O

R-COOH, R-CO2H, R C

OH





Common names:

HCO2H formic acid L. formica ant

CH3CO2H acetic acid L. acetum vinegar

CH3CH2CO2H propionic acid G. “first salt”

CH3CH2CH2CO2H butyric acid L. butyrum butter

CH3CH2CH2CH2CO2H valeric acid L. valerans

Carboxylic acids, common names:



CH3(CH2)4CO2H caproic acid L. caper goat

CH3(CH2)5CO2H ---

CH3(CH2)6CO2H caprylic acid

CH3(CH2)7CO2H ---

CH3(CH2)8CO2H capric acid

CH3(CH2)9CO2H ---

CH3(CH2)10CO2H lauric acid oil of lauryl

5 4 3 2 1

C—C—C—C—C=O

δ γ β α used in common names



Br CH3

CH3CH2CH2CHCOOH CH3CHCH2COOH



 bromovaleric acid  -methylbutyric acid

isovaleric acid

COOH

special names

benzoic acid







COOH COOH COOH

CH3



CH3

CH3



o-toluic acid m-toluic acid p-toluic acid

IUPAC nomenclature for carboxylic acids:

parent chain = longest, continuous carbon chain that contains

the carboxyl group  alkane, drop –e, add –oic acid





HCOOH methanoic acid

CH3CO2H ethanoic acid

CH3CH2CO2H propanoic acid





CH3

CH3CHCOOH 2-methylpropanoic acid



Br

CH3CH2CHCO2H 2-bromobutanoic acid

dicarboxylic acids:

HOOC-COOH oxalic acid

HO2C-CH2-CO2H malonic acid

HO2C-CH2CH2-CO2H succinic acid

HO2C-CH2CH2CH2-CO2H glutaric acid

HOOC-(CH2)4-COOH adipic acid

HOOC-(CH2)5-COOH pimelic acid





Oh, my! Such good apple pie!

CO2H CO2H

CO2H



CO2H CO2H

CO2H

phthalic acid isophthalic acid

terephthalic acid









H COOH H COOH

C C

C C

H COOH HOOC H



maleic acid fumaric acid

salts of carboxylic acids:

name of cation + name of acid: drop –ic acid, add –ate





CH3CO2Na sodium acetate or sodium ethanoate





CH3CH2CH2CO2NH4 ammonium butyrate

ammonium butanoate





(CH3CH2COO)2Mg magnesium propionate

magnesium propanoate

O O

C C

HO OH HO ONa



carbonic acid sodium bicarbonate

sodium hydrogen carbonate

NaHCO3

O

C

NaO ONa

sodium carbonate



Na2CO3

physical properties:

polar + hydrogen bond  relatively high mp/bp

water insoluble

exceptions: four carbons or less

acidic turn blue litmus  red

soluble in 5% NaOH





RCO2H + NaOH  RCO2-Na+ + H2O

stronger stronger weaker weaker

acid base base acid

RCO2H RCO2-

covalent ionic

water insoluble water soluble



Carboxylic acids are insoluble in water, but soluble in 5%

NaOH.



1. Identification.

2. Separation of carboxylic acids from basic/neutral organic

compounds.

The carboxylic acid can be extracted with aq. NaOH and

then regenerated by the addition of strong acid.

Carboxylic acids, syntheses:

1. oxidation of primary alcohols

RCH2OH + K2Cr2O7  RCOOH

2. oxidation of arenes

ArR + KMnO4, heat  ArCOOH

3. carbonation of Grignard reagents

RMgX + CO2  RCO2MgX + H+ 

RCOOH

4. hydrolysis of nitriles

RCN + H2O, H+, heat  RCOOH

1. oxidation of 1o alcohols:







CH3CH2CH2CH2-OH + CrO3  CH3CH2CH2CO2H

n-butyl alcohol butyric acid

1-butanol butanoic acid





CH3 CH3

CH3CHCH2-OH + KMnO4  CH3CHCOOH

isobutyl alcohol isobutyric acid

2-methyl-1-propanol` 2-methylpropanoic acid

2. oxidation of arenes:

KMnO4, heat

CH3 COOH



toluene benzoic acid







CH3 COOH note: aromatic

KMnO4, heat

acids only!



H3C HOOC



p-xylene terephthalic acid







KMnO4, heat

CH2CH3 COOH + CO2



ethylbenzene benzoic acid

3. carbonation of Grignard reagent:



Mg CO2 H+

R-X RMgX RCO2MgX RCOOH

Increases the carbon chain by one carbon.



Mg CO2 H+

CH3CH2CH2-Br CH3CH2CH2MgBr CH3CH2CH2COOH

n-propyl bromide butyric acid



H+

O O O

+ +MgX

RMgX + C R C R C

O- OH

O

CH3 CH3 CH3

Mg CO2 H+





Br MgBr COOH



p-toluic acid





Br2, hv Mg

CH3 CH2Br CH2MgBr





CO2



H+





CH2 COOH





phenylacetic acid

4. Hydrolysis of a nitrile:





H2O, H+

R-CN R-CO2H

heat



H2O, OH-

R-CN R-CO2- + H+  R-CO2H

heat



R-X + NaCN  R-CN + H+, H2O, heat  RCOOH

1o alkyl halide



Adds one more carbon to the chain.

R-X must be 1o or CH3!

Br2, hv NaCN

CH3 CH2Br CH2 CN



toluene

H2O, H+, heat





CH2 COOH



phenylacetic acid



KCN

CH3CH2CH2CH2CH2CH2-Br CH3CH2CH2CH2CH2CH2-CN

1-bromohexane

H2O, H+, heat





CH3CH2CH2CH2CH2CH2-COOH

heptanoic acid

CH2OH



KMnO4







CH3

KMnO4, heat

CO2H





Br MgBr

Mg

CO2; then H+









C N

H2O, H+, heat

carboxylic acids, reactions:

1. as acids

2. conversion into functional derivatives

a)  acid chlorides

b)  esters

c)  amides

3. reduction

4. alpha-halogenation

5. EAS

as acids:

a) with active metals

RCO2H + Na  RCO2-Na+ + H2(g)

b) with bases

RCO2H + NaOH  RCO2-Na+ + H2O

c) relative acid strength?

CH4 < NH3 < HCCH < ROH < HOH < H2CO3 < RCO2H < HF

d) quantitative

HA + H2O  H3O+ + A- ionization in water

Ka = [H3O+] [A-] / [HA]

Ka for carboxylic acids  10-5

Why are carboxylic acids more acidic than alcohols?

ROH + H2O  H3O+ + RO-

RCOOH + H2O  H3O+ + RCOO-

ΔGo = -2.303 R T log Keq

The position of the equilibrium is determined by the free energy

change, ΔGo.

ΔGo = ΔH - TΔS

ΔGo  ΔH Ka is inversely related to ΔH, the potential

energy difference between the acid and its conjugate base. The

smaller the ΔH, the larger the Ka and the stronger the acid.

potential energy H3O+ + A-









ΔH





HA + H2O







ionization







The smaller the ΔH, the more the equilibrium lies to the

right, giving a larger Ka ( a stronger acid ).

O O-

R C R C

O- O







O

R C

O





Resonance stabilization of the carboxylate ion decreases

the ΔH, shifts the ionization in water to the right, increases

the Ka, and results in carboxylic acids being stronger acids.

Effect of substituent groups on acid strength?





CH3COOH 1.75 x 10-5

ClCH2COOH 136 x 10-5

Cl2CHCOOH 5,530 x 10-5

Cl3CCOOH 23,200 x 10-5





-Cl is electron withdrawing and delocalizes the negative

charge on the carboxylate ion, lowering the PE, decreasing

the ΔH, shifting the ionization to the right and increasing

acid strength.

Effect of substituent groups on acid strength of benzoic acids?





Electron withdrawing groups will stabilize the anion, decrease the ΔH, shift

the ionization to the right, increasing the Ka, increasing acid strength.



COO-



G





Electron donating groups will destabilize the anion, increase the ΔH, shift the

ionization in water to the left, decreasing the Ka, decreasing acid strength.



COO-



G

-NH2, -NHR, -NR2

-OH

-OR electron donating

-NHCOCH3

-C6H5

-R

-H

-X

-CHO, -COR

-SO3H

-COOH, -COOR electron withdrawing

-CN

-NR3+

-NO2

Relative acid strength?

Ka

p-aminobenzoic acid 1.4 x 10-5

p-hydroxybenzoic acid 2.6 x 10-5

p-methoxybenzoic acid 3.3 x 10-5

p-toluic acid 4.2 x 10-5

benzoic acid 6.3 x 10-5

p-chlorobenzoic acid 10.3 x 10-5

p-nitrobenzoic acid 36 x 10-5

2. Conversion into functional derivatives:

a)  acid chlorides



O SOCl2 O

R C R C

OH or PCl3 Cl

orPCl5







CO2H + SOCl2 COCl







O PCl3 O

CH3CH2CH2 C CH3CH2CH2 C

OH Cl

b)  esters

―direct‖ esterification: H+

RCOOH + R´OH  RCO2R´ + H2O

-reversible and often does not favor the ester

-use an excess of the alcohol or acid to shift equilibrium

-or remove the products to shift equilibrium to completion





―indirect‖ esterification:

RCOOH + PCl3  RCOCl + R´OH  RCO2R´

-convert the acid into the acid chloride first; not reversible

O H+ O

C + CH3OH C + H2O

OH O CH3



SOCl2







O CH3OH

C

Cl

c)  amides

―indirect‖ only!

RCOOH + SOCl2  RCOCl + NH3  RCONH2

amide

O O

PCl3 NH3 O

OH Cl NH2

3-Methylbutanoic acid





Directly reacting ammonia with a carboxylic acid results in an

ammonium salt:

RCOOH + NH3  RCOO-NH4+

acid base

O PCl3 O NH3 O

C C C

OH Cl NH2



amide



NH3







O

C ammonium salt

O NH4

3. Reduction:

RCO2H + LiAlH4; then H+  RCH2OH

1o alcohol



LiAlH4 H+

CH3CH2CH2CH2CH2CH2CH2COOH

Octanoic acid

(Caprylic acid)

CH3CH2CH2CH2CH2CH2CH2CH2OH

1-Octanol









Carboxylic acids resist catalytic reduction under normal

conditions.

RCOOH + H2, Ni  NR

O H2, Pt

CH2 C NR

OH



LiAlH4



H+







CH2CH2OH

4. Alpha-halogenation: (Hell-Volhard-Zelinsky reaction)



RCH2COOH + X2, P  RCHCOOH + HX

X

α-haloacid

X2 = Cl2, Br2





CH3CH2CH2CH2COOH + Br2,P CH3CH2CH2CHCOOH

pentanoic acid Br

2-bromopentanoic acid



COOH

Br2,P

NR (no alpha H)

RCH2COOH + Br2,P RCHCOOH + HBr

+ Br

nH

; the

OH NH3

Na





RCHCOOH RCHCOOH

aminoacid

NH2

OH







KOH(alc)

RCH2CHCOOH RCH=CHCOOH

Br then H+

5. EAS: (-COOH is deactivating and meta- directing)

CO2H

HNO3,H2SO4



NO2



CO2H

H2SO4,SO3

CO2H



SO3H



CO2H

benzoic acid Br2,Fe



Br





CH3Cl,AlCl3

NR

spectroscopy:





IR: -COOH O—H stretch 2500 – 3000 cm-1 (b)

C=O stretch 1680 – 1725 (s)





nmr: -COOH 10.5 – 12 ppm

p-toluic acid









-COO—H

stretch

C=O

COOH c



b





CH3 a









c b a

Carboxylic acids, syntheses:

1. oxidation of primary alcohols

RCH2OH + K2Cr2O7  RCOOH

2. oxidation of arenes

ArR + KMnO4, heat  ArCOOH

3. carbonation of Grignard reagents

RMgX + CO2  RCO2MgX + H+ 

RCOOH

4. hydrolysis of nitriles

RCN + H2O, H+, heat  RCOOH

carboxylic acids, reactions:

1. as acids

2. conversion into functional derivatives

a)  acid chlorides

b)  esters

c)  amides

3. reduction

4. alpha-halogenation

5. EAS


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