Structure-Acidity Relationships

Introduction

In our discussion of acid-base equilibria, we saw how to calculate the equilibrium constant for any reaction involving two acids of known acid strength. By comparing differences in acidity within carefully selected groups of structurally related compounds, it is possible to gain insight into the relationship between molecular structure and chemical reactivity. In this topic we will make correlations between changes in pKa values and various atomic, molecular, and experimental variables:

We'll start by looking at HF and its relatives, H2O, NH3, and CH4.

Charge Stability and Electronegativity

Equation 1 describes the general reaction that we want to consider.


Exercise 1 The following table lists four different compounds that fit the formula HA along with some additional information. Complete the table. Enter an exponential value such as 10-6 as 10e-6.

HA

pKa

Keq

-:A

Atomic number of the central atom

Bond Energy, kcal/mol

CH4

-:CH3, methide ion

104

NH3

-:NH2, amide ion

103

H2O

-:OH, hydroxide ion

119

HF

-:F, fluoride ion

136


In all of these reactions the reactants are neutral while the products bear formal charges. It seems reasonable to attribute changes in the pKa and Keq values to variations in the ability of the negatively charged atom to accomodate the negative charge.
Exercise 2 The central atom of each of the conjugate bases in the table has a filled valence shell. The ratio of nuclear charge to number of valence shell electrons is 6:8 in methide ion. What is this ratio in amide ion? What is it in hydroxide ion? What is it in fluoride ion?

Exercise 3 The ion -:A is most stable when A equals . Of the four compounds listed in the table, is the strongest acid. This is because ion is the most stable conjugate base.

Exercise 4 The ion -:A is least stable when A equals . Of the four compounds listed in the table, is the weakest acid. This is because ion is the least stable conjugate base.


All of the central atoms in these four compounds have the same valence shell, namely n = 2. Now let's consider a series of four compounds in which n varies from 2 to 3 to 4 to 5, namely the hydrogen halides.

Relative Acidities of the Hydrogen Halides

In aqueous solution the relative acidities of the hydrogen halides is HI > HBr > HCl > HF.


Exercise 5 Complete the following table. Enter an exponential value such as 10-6 as 10e-6.

HA

pKa

Keq

-:A

Atomic radius of A, pm

HA BondStrength, kcal/mol

HF

-:F, fluoride ion

72

136

HCl

-:Cl, chloride ion

99

103

HBr

-:Br, bromide ion

114

88

HI

-:I, iodide ion

133

71

Exercise 6 In the hydrogen halides, there is adirect inverse correlation between the atomic radius of the halogen atom and the strength of the hydrogen-halogen bond.

Exercise 7 In the hydrogen halides, there is a direct inverse correlation between the bond strength and the pKa value.

Exercise 8 In the hydrogen halides, there is a direct inverse correlation between the H-A bond strength and the acidity of HA.


It should be clear that the balance of factors which contribute to trends in acidity as you go across a row in the periodic table is different than the balance that determines the relative acidities as you go down a group. The bottom line is that you have to be flexible. Although there are no hard and fast rules to go by, the trends can generally be rationalized in terms of the balance between two factors or three factors. The last factor we will examine in this topic is resonance.

Charge Stability and Resonance

Figure 1 compares the dissociation reactions of methanol and phenol. As you can see, phenol is approximately 1,000,000 times more acidic than methanol. Clearly differences in bond strengths or electronegativity are not responsible for this difference in acidity since an O-H bond is broken in both cases and the negative charge resides on an oxygen atom in both conjugate bases.

Figure 1

Resonance to the Rescue

In our discussion of resonance theory we saw that when an orbital containing a lone pair of electrons can overlap with a p orbital of an adjacent multiple bond as shown in Figure 2, the energy of the system decreases.

Figure 2

If the Shoe Fits..

As Figure 3 indicates, the phenolate ion, C6H5O:-, meets this structural requirement.

Figure 3

Lending a Helping Hand

Notice that Figure implies that the orbital overlap leads to changes in the hybridization of the oxygen atom. This change decreases the separation between the orbitals on the oxygen and the adjacent carbon and increases their overlap.


Exercise 9 In Figure 3 the hybridization of the oxygen atom changes fromto.

This orbital overlap leads to charge delocalization as indicated by the resonance structures shown in Figure 4.

Figure 4

Spread 'em Out


Exercise 10 Following the formalism shown in Figure 4, draw structural diagrams to indicate the transfer of negative charge from the carbon in representation D to the oxygen in representation A.
Now consider the difference in pKa values of methanol and acetic acid. Figure 5 provides a comparison.

Figure 5

Here We Go Again

As you can see, the O-H hydrogen in acetic acid is 11 orders of magnitude more acidic than that in methanol. Conversely, the methoxide ion, CH3O:-, is 11 orders of magnitude more basic than the acetate ion. Clearly the carbonyl group affects the acidity of the adjacent O-H group dramatically. We attribute this increase in acidity to the stabilization that the double bond affords the negative charge as it develops in the conjugate base of acetic acid. The interaction between a lone pair of electrons on the oxygen and the adjacent carbonyl group is shown in Figure 6.

Figure 6

Spread 'em Again

Remember, the formalism shown in Figure 6 is our way of indicating that the negative charge in the acetate ion can experience the nuclear attraction of both oxygen atoms. This increase in Coulombic attraction reduces the potential energy of the acetate ion relative to that of the methoxide ion where the charge is localized on one oxygen atom.


Exercise 11 Draw a picture similar to the one shown in Figure 3 to show the overlap of orbitals that is implied in Figure 6.

Exercise 12 The pKa of ethane is approximately 50 while that of acetone is about 20. Write equations similar to Equation 1 for each of these compounds. Explain why acetone is 30 powers of 10 more acidic than ethane. Draw resonance structures and orbital diagrams to illustrate your answer.

Exercise 13 What is the equilibrium constant for the following reaction?


Topics