Explain in details the Some objects are not the same as their mirror images (technically, they have no plane of symmetry)
A right-hand glove is different than a left-hand glove. The property is commonly called “handedness”
Organic molecules (including many drugs) have handedness that results from substitution patterns on sp3 hybridized carbon
2
Stereochemistry
Some objectsare not the
same as their mirror
images (technically, they
have no plane of
symmetry)
A right-hand glove is
different than a left-
hand glove. The
property is commonly
called “handedness”
Organic molecules
(including many drugs)
have handedness that
results from substitution
patterns on sp3
hybridized
carbon
3.
3
Why this Chapter?
Handedness is important in organic and
biochemistry
Molecular handedness makes possible
specific interactions between enzymes and
substrates
Stereochemistry looks at 3-D structures of
molecules
4.
4
9.1 Enantiomers andthe Tetrahedral
Carbon
Enantiomers are molecules that are not the same as
their mirror image
They are the “same” if the positions of the atoms can
coincide on a one-to-one basis (we test if they are
superimposable, which is imaginary)
This is illustrated by enantiomers of lactic acid
5.
5
Examples of Enantiomers
Molecules that have one carbon with 4
different substituents have a
nonsuperimposable mirror image – enantiomer
6.
6
9.2 The Reasonfor Handedness:
Chirality
Molecules that are not superimposable with their
mirror images are chiral (have handedness)
A plane of symmetry divides an entire molecule
into two pieces that are exact mirror images
A molecule with a plane of symmetry is the same as
its mirror image and is said to be achiral
7.
7
Chirality
If anobject has a plane of symmetry it is necessarily
the same as its mirror image
The lack of a plane of symmetry is called
“handedness”, chirality
Hands, gloves are prime examples of chiral object
They have a “left” and a “right” version
8.
8
Plane of Symmetry
The plane has the same
thing on both sides for
the flask
There is no mirror plane
for a hand
9.
9
Chirality Centers
Apoint in a molecule where four different groups (or
atoms) are attached to carbon is called a chirality center
There are two nonsuperimposable ways that 4 different
different groups (or atoms) can be attached to one carbon
atom
If two groups are the same, then there is only one way
A chiral molecule usually has at least one chirality center
10.
10
Chirality Centers inChiral Molecules
Groups are considered “different” if there is any
structural variation (if the groups could not be
superimposed if detached, they are different)
In cyclic molecules, we compare by following in each
direction in a ring
11.
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9.3 Optical Activity
Light restricted to pass through a plane is plane-
polarized
Plane-polarized light that passes through solutions of
achiral compounds remains in that plane
Solutions of chiral compounds rotate plane-polarized
light and the molecules are said to be optically active
Phenomenon discovered by Jean-Baptiste Biot in the
early 19th
century
12.
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Optical Activity
Lightpasses through a plane polarizer
Plane polarized light is rotated in solutions of optically
active compounds
Measured with polarimeter
Rotation, in degrees, is []
Clockwise rotation is called dextrorotatory
Anti-clockwise is levorotatory
13.
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Measurement of Optical
Rotation
A polarimeter measures the rotation of plane-
polarized that has passed through a solution
The source passes through a polarizer and then is
detected at a second polarizer
The angle between the entrance and exit planes is
the optical rotation.
14.
14
Polarimetry
Use monochromaticlight, usually sodium D
Movable polarizing filter to measure angle
Clockwise = dextrorotatory = d or (+)
Counterclockwise = levorotatory = l or (-)
Not related to (R) and (S)
=>
15.
15
Specific Rotation
Tohave a basis for comparison, define specific
rotation, []D for an optically active compound
[]D = observed rotation/(pathlength x concentration)
= /(l x C) = degrees/(dm x g/mL)
Specific rotation is that observed for 1 g/mL in
solution in cell with a 10 cm path using light from
sodium metal vapor (589 nm)
16.
16
Specific Rotation andMolecules
Characteristic property of a compound that is optically active – the
compound must be chiral
The specific rotation of the enantiomer is equal in magnitude but
opposite in sign
17.
17
9.5 Sequence Rulesfor
Specification of Configuration
A general method applies to the configuration at each
chirality center (instead of to the whole molecule)
The configuration is specified by the relative positions
of all the groups with respect to each other at the
chirality center
The groups are ranked in an established priority
sequence and compared
The relationship of the groups in priority order in
space determines the label applied to the
configuration, according to a rule
18.
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Sequence Rules (IUPAC)
Rule1:
• Assign each group priority according to the Cahn
Ingold-Prelog scheme
• With the lowest priority group pointing away, look
at remaining 3 groups in a plane
• Clockwise is designated R (from Latin for “right”)
• Counterclockwise is designated S (from Latin word
for “left”)
19.
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Rule 2:
Ifdecision can’t be reached by ranking the first atoms
in the substituents, look at the second, third, or fourth
atoms until difference is found
24
9.6 Diastereomers
Moleculeswith more than one chirality center have
mirror image stereoisomers that are enantiomers
In addition they can have stereoisomeric forms that are
not mirror images, called diastereomers
26
9.7 Meso Compounds
Tartaric acid has two chirality centers and two diastereomeric
forms
One form is chiral and the other is achiral, but both have two
chirality centers
An achiral compound with chirality centers is called a meso
compound – it has a plane of symmetry
The two structures on the right in the figure are identical so the
compound (2R, 3S) is achiral
27.
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9.8 Racemic Mixturesand The
Resolution of Enantiomers
A 50:50 mixture of two chiral compounds that are
mirror images does not rotate light – called a
racemic mixture (named for “racemic acid” that was
the double salt of (+) and (-) tartaric acid
The pure compounds need to be separated or
resolved from the mixture (called a racemate)
To separate components of a racemate (reversibly)
we make a derivative of each with a chiral substance
that is free of its enantiomer (resolving agent)
This gives diastereomers that are separated by their
differing solubility
The resolving agent is then removed
30
Fischer Projections
Flatdrawing that represents a 3D molecule
A chiral carbon is at the intersection of horizontal and
vertical lines.
Horizontal lines are forward, out-of-plane.
Vertical lines are behind the plane.
31.
31
Fischer Rules
Carbonchain is on the vertical line.
Highest oxidized carbon at top.
Rotation of 180 in plane doesn’t change
molecule.
Do not rotate 90!
Do not turn over out of plane! =>
32.
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Fischer Mirror Images
Easy to draw, easy to find enantiomers, easy
to find internal mirror planes.
Examples:
CH3
H Cl
Cl H
CH3
CH3
Cl H
H Cl
CH3
CH3
H Cl
H Cl
CH3
=>
33.
33
Fischer (R) and(S)
Lowest priority (usually H) comes forward, so
assignment rules are backwards!
Clockwise 1-2-3 is (S) and counterclockwise 1-2-3 is
(R).
Example:
CH3
H Cl
Cl H
CH3
(S)
(S) =>
35
Alkenes
Cis-trans isomers arenot mirror images, so
these are diastereomers.
C C
H H
CH3
H3C
cis-2-butene trans-2-butene
C C
H
H3C
CH3
H =>
36.
36
Ring Compounds
Cis-transisomers possible.
May also have enantiomers.
Example: trans-1,3-dimethylcylohexane
CH3
H
H
CH3
CH3
H
H
CH3
=>
37.
37
Two or MoreChiral Carbons
Enantiomer? Diastereomer? Meso? Assign (R) or
(S) to each chiral carbon.
Enantiomers have opposite configurations at each
corresponding chiral carbon.
Diastereomers have some matching, some opposite
configurations.
Meso compounds have internal mirror plane.
Maximum number is 2n
, where n = the number of
chiral carbons.
=>
41
Stereoisomers
Same connections,different spatial arrangement of atoms
Enantiomers (nonsuperimposable mirror images)
Diastereomers (all other stereoisomers)
Includes cis, trans and configurational