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Diels-Alder Rxn Stereochemistry

1

2

3

4

Diene

Dienophile

Reflux

High BP Solvent

(110oC)

5

6

5

4

3

2

1

6

(Click “Slideshow” to Animate)

6-Carbon Ring

(Cyclohexene)

Nobel Prize in Chem. 1950

First we’ll look at a simple Diels-Alder Reaction that has no Stereochemistry.

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Diels-Alder Rxn Stereochemistry

1

2

3

4

5

6

Diene

Dienophile

Out

Out

Cis Dienophile

Out, Out

Cis Prod.

Cis Prod.

Cis Prod.

Cis Prod.

Cis Prod.

Cis Prod.

1

2

3

4

5

6

Not Mirror Images

Diastereomers

Same MF

Non-Superimposable

Same Connectivity

Achiral Diene

Achiral Dienophile

Meso

Achiral Product

Meso

Achiral Product

Achiral Reactants

Achiral

Product Mixture

Achiral

Solvent

Reflux

High BP Solvent

(110oC)

=

=

Nobel Prize in Chem. 1950

Now to add Stereochemistry…

Diastereomers

Pancake Flip

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Diels-Alder Rxn Stereochemistry

In, Out

Alkyne

Trans

Trans

Trans Prod.

Out

In

Will not make Stereocenters

Achiral Diene

Achiral Dienophile

Achiral Reactants

Achiral

Solvent

Chiral Product

Achiral

Product Mixture

Chiral Product

50%

50%

Enantiomers

Racemic Mix.

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Diels-Alder Rxn Stereochemistry

In, Out, In, Out

Trans Dienophile

Trans

Trans

Will not make Stereocenters

Trans Prod.

Racemic Mixture of Enantiomers

Rotate Diene to visualize mechanism better.

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Diels-Alder Rxn Stereochemistry

=

=

In, In

Trans

Cis

Trans

Cis

Trans

Racemic Mixture of Enantiomers

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Diels-Alder Rxn Stereochemistry

Endo

Exo

Major

Minor

1

2

3

4

5

6

1

2

3

4

5

A

6

B

A

B

Unequal Mixture of Diastereomers

Rotate Diene and Dienophile to visualize mechanism better.

Achiral

Diene

Achiral

Dienophile

Achiral

Solvent

Both Products Meso

Both Achiral

Achiral

Reactants

Achiral

Products

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Diels-Alder Rxn Stereochemistry

In, In

Trans

In, In

Trans

In, In

Trans

This Ketone

is Endo

This Ketone

is Endo

This Ketone

is Exo

This Ketone

is Exo

Neither Product is overall Exo or Endo

Racemic Mixture of Enantiomers

Achiral Reactants → Achiral Product Mixture