2 chirality and projection 25 10 2013 [compatibility mode]

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Geometrical cis-trans and E-/Z-isomers Such isomers contain double bonds, which cannot rotate They can also arise from ring structures, wherein the rotation of bonds is greatly restricted

Nomenclature Rules CIP (Cahn-Ingold-Prelog): - ranking all substituents according to atomic number - in case of identical atoms go to the next / adjacent atom 4


Cis isomers

Trans isomers

The same groups are

The same groups are

on the same side of

on opposite sides of the

the C=C bond

C=C bond

Chapter 4


Cis but-2-ene

trans but-2-ene


Geometric isomerism

H

H C=C

H

does not exist in symmetrical alkenes

CH2CH3

But-1-ene

because one C has two identical groups attached


Cis-trans isomers are not mirror images, so these are diastereomers. H

H

CH3 C C

C C H3C

H

CH3

cis-2-butene

H3C H trans-2-butene

DiastereomerďźšIsomers that are non superimposable, not mirror images. 8


The E-Z convention for Cis-Trans Isomers


Br

Br C

CH3

CH3

Br

C

C

H

H

H

C C

C

H

Br

C

C

H

CH3

Br

Br H3C

C

CH3

Br

Br CH3 H

cis-1,2-dimethyl-3,3-dibromocyclopropane

H3C H

C C

H C CH3

trans-1,2-dimethyl-3,3-dibromocyclopropane


Different compounds- different properties.


Conformation (Rotation of C-C Single Bonds) Conformations are different arrangements of atoms that are interconverted by rotation about single bonds. Different conformations also are called conformational isomers or conformers:

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Conformations of Alkanes: Rotation of C-C Single Bonds

13


Newman projection How to Draw a Newman Projection: Step 1. Look directly down the C—C bond (end-on), and draw a circle with a dot in the center to represent the carbons of the C—C bond.

14


Step 2. Draw the bonds on the front C as three lines meeting at the center of the circle. Draw the bonds on the back C as three lines coming out of the edge of the circle.

Step 3. Add the atoms on each bond.

15


16


• In the eclipsed conformation, the C—H bonds on one carbon are directly aligned with the C—H bonds on the adjacent carbon. • In the staggered conformation, the C—H bonds on one carbon bisect the H—C—H bond angle on the adjacent carbon. • The staggered conformations are more stable than the eclipsed conformations. • Electron-electron repulsion between bonds in the eclipsed conformation increases its energy compared with the staggered conformation.

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• An energy minimum and maximum occur every 60° as the conformation changes from staggered to eclipsed. Conformations that are neither staggered nor eclipsed are intermediate in energy. • Butane and higher molecular weight alkanes have several C—C bonds, all capable of rotation. It takes six 60° rotations to return to the original conformation.

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A staggered conformation with two larger groups 180째 from each other is called anti. A staggered conformation with two larger groups 60째 from each other is called gauche. The staggered conformations are lower in energy than the eclipsed conformations. Steric strain is an increase in energy resulting when atoms are forced too close to one another. Gauche conformations are generally higher in energy than anti conformations because of steric strain.

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Conformations of Butane: Rotation of C2-C3 Single Bond

20


Drawing Cyclohexane



Numbering Cyclohexane

Start anywhere and number consecutive carbons.


hold red bonds in a plane, flip this carbon above the plane. flip the other carbon below the plane you get the other chair conformation.


How to draw the two conformations of

a substituted

cyclohexane: • The two conformations of cyclohexane are different, so they are not equally stable. • Larger axial substituents create unfavorable 1,3-diaxial interactions. • In methylcyclohexane, each unfavorable H,CH3 interaction destabilizes the conformation by 0.9 kcal/mol, so Conformation 2 is 1.8 kcal/mol less stable than Conformation 1.


Substituted Cyclohexane • The larger the substituent on the six-membered ring, the higher the percentage of the conformation containing the equatorial substituent. • With a very large substituent like tert-butyl [(CH3)3C-], essentially none of the conformation containing an axial tert-butyl group is present at room temperature, so the ring is essentially anchored in a single conformation having an equatorial tert-butyl group.


5

up

up 6

down

up 1

up

2

3

down down

up

4 down

4

up

up

up

up

up

down down

5

6 down

down up

1

2 3

down

down

down down

Each carbon has two groups (up and down) cis: When the two groups are on the same side, either both on up bonds or both on down bonds.

trans: When the two groups on opposite sides, one up and one down.

up



trans-1,4-dimethylcyclohexane

The two conformations have one methyl up and one methyl down. Conformations 1 and 2 are not equally stable because conformation 2 has both larger CH3 groups in the equatorial position, it is lower in energy.


cis-1,4-dimethylcyclohexane

The two conformations have the two methyl groups drawn up Both conformations have one methyl group axial and one equatorial, making them equally stable.


Optical isomerism Chirality

Chapter 4


Chiral objects don’t have a plane of symmetry. symmetry

Objects with a plane of symmetry are achiral.

Problem 2.2: chiral objects achiral (non chiral) objects • screw, scissors nail, knife • glove, shoe, jacket sock, pullover • your hand, foot, ear, nose, yourself

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Configuration Isomers: Isomers with One Chirality Center

A chirality center arises when four

different

substituents

are bonded to a carbon.

33


Two

enantiomers

nonsuperimposable images of each other

are mirror (as

right and left hand).

34


Drawing Enantiomers Perspective Formulas:

35


Naming Enantiomers: The R,S System Cahn, Ingold, Prelog sequence rules: The atom attached to the chiral center with the highest atomic number = 1, next = 2, etc. If the four atoms attached to the chiral center are not all different, the sequence is determined at the first point of difference. The multiply bonded atom as an equivalent number of singly bonded atoms (For example, the C of a C=O is considered to be bonded to two O atoms)

Rotate the number 4 group away from you and observe the sequence 1 3 for the remaining groups. If going from 1

2

If going from 1

2

2

3 is clockwise, then the configuration is R (rectus). 3 is anti-clockwise, then the configuration is S (sinister).


Examples of assigning priorities to stereogenic centers

1

4 2

3

(S)-2-bromobutane

37


1

2 3 R

2

1 3 S

Orienting the lowest priority group in back

R


If group of lowest priority is not bonded by a hatched wedge, switch a pair of groups so that the group of lowest priority is bonded by the hatched wedge: Any one exchange of groups around a stereocenter produces the other stereoisomer Any even number of exchange of groups around a stereocenter produces the original configuration


In drawing arrow from 1 to 2, you can draw past the group of lowest priority (4), but never draw past the group of priority (3):


Optical Rotation

[α ] = Τ λ

α lxc

T = temperature [°C] λ = wavelength [nm] α = measured rotation [°] l = path length [dm] c = concentration [g/mL]

[α ]Tλ = specific rotation 41


Optical Rotation and Absolute Configuration In general there is no relationship between the R or S configuration of an enantiomer and the direction it rotates polarized light. This must be determined by experiment: CH3

CH3 H

H OH

COOH

(S)-(+)-lactic acid

OH

COO-Na+

(S)-(–)-sodium lactate

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Racemic mixture (racemate) A mixture of equal amounts of two enantiomers is called a racemic mixture (racemate) A racemic mixture is denoted by the prefix (Âą) or dl indicating an equal (1:1) mixture of dextro and levo isomers Also the prefix rac- (or racem-) or the symbols RS and SR are used A racemate is optically inactive, meaning that there is no net rotation of plane-polarized light. Although the two enantiomers rotate planepolarized light in opposite directions, the rotations cancel because they are present in equal amounts.

Chapter 4


R and S configuration Indicate whether the structure has R or S configuration: 2 CH(CH3)2

4

C

CH3

3 CH2CH3

switch CH3 and CH3CH2

CH2Br 1

R 44



Drawing Enantiomers Fischer Projections: vertical bonds horizontal bonds

substituents directed away from the observer substituents dircted toward the observer

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Fischer Guidelines 1. Fischer formulas may only be rotated 180o in the plane of the paper 2. Any even number of exchange of groups around a stereocenter produces the original configuration 3. Any one exchange of groups around a stereocenter produces the other stereoisomer (R

S, S

R)

4. If manipulation outlined in 2 or 3 allows one Fischer projection to superimpose on another, they are the same steroisomer



Fischer projections

transform molecule to eclipsed conformation in order to construct Fischer projection


The R,S System in case of Fischer projection If the group of lowest priority is on a vertical line, just draw the curve according to decreasing priority. Clockwise

- configuration is R.

Counterclockwise - configuration is S.

(S)-2-bromobutane 50


If the group of lowest priority is on a horizontal line, just draw the curve according to decreasing priority. Clockwise

- configuration is S.

Counterclockwise - configuration is R.

(R)-2-bromobutane 51


Naming Enantiomers: The R,S System Working

with

Fischer

Projections, a rotation of 90째 or a horizontal flip will switch

(R)-2-bromobutane (S)-2-bromobutane

chirality.

(R)-2-bromobutane (S)-2-bromobutane Rotation

of

a

Fischer

projection by 180째in the plane of the paper does not switch the chirality.

(R)-2-bromobutane (R)-2-bromobutane 52


In each case, assign the correct configuration ( R or S) ? To simplify the problem, we convert the three dimension structure into Fisher projection, as follow:

4

2

4 3

1

1

3

4

2

S 1

1 2

3

1

2 4

1

3

3

4

S

4

2 4

3 1

2

4

2 1

3

1

4

4

3

2

4

4

R 1

3

1

2

3

3

1

4

3

R

2

4

4

2

2 4

3

3

2

1

S

2 2

1

2

3

1

4

2

2 1

3

R

3 1

4

1 3


1

2

3

2

3 1 4

4

4 1 2

3

4

1

3

2

4

2

1

3

2

1

R 3

4

1

1 3 2

2 3 4

4 4

2

1

1

2

3 4

3

R 3

1

4

4 3 2

S

2 3 1

2

1

4

2 4

1

2

3

4 3

1


Compounds with more than one chiral center


Three stereoisomers of 2,3-butanediol

2R,3R

2S,3S

2R,3S

chiral

chiral

achiral


Three stereoisomers of 2,3-butanediol


2R,3R

2S,3S

chiral

chiral

enantiomers


meso-compound

CH3 H

OH

H

OH CH3 2R,3S

2R,3S

achiral

meso forms have a plane of symmetry and/or a center of symmetry The top half of the molecule is mirror image of the bottom half


Other Examples

meso-compound – a compound that has chiral centers but is not chiral (optically inactive).


Erythro and Threo They are diastereomers with two adjacent chiral Carbons, without symmetric ends

Threo isomer

Erythro isomer They have two similar substituents

They have two similar substituents on the opposite side

on the same side

CH2CH3

X CH2CH3

X H

H

R R

H

H

R

Br

e.g. H

R H

e.g.

Br

H

H

Br

Br

Y Y erythro X#Y

CH3

CH3 threo erythro-2,3-dibromopentane

threo-2,3-dibromopentane

X#Y

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Example 2: 2,3-dichloropentane



Conversion of Newman into sawhrose and Fisher projection

Chapter 4


Conversion of Perspective into Fisher projection D

A B A

C

D

B

C

F

E

E F

E

F

C

B

D

Top left view

A

bottom right view


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