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Drug Synthesis

The document outlines various methods of drug synthesis, focusing on alkanes, alkenes, alcohols, ethers, aldehydes, ketones, and amines. It describes the general formulas, industrial sources, and specific reactions involved in synthesizing these compounds, including Grignard synthesis and oxidation processes. Additionally, it covers electrophilic aromatic substitutions and various condensation reactions relevant to organic chemistry.

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keenallan08
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13 views116 pages

Drug Synthesis

The document outlines various methods of drug synthesis, focusing on alkanes, alkenes, alcohols, ethers, aldehydes, ketones, and amines. It describes the general formulas, industrial sources, and specific reactions involved in synthesizing these compounds, including Grignard synthesis and oxidation processes. Additionally, it covers electrophilic aromatic substitutions and various condensation reactions relevant to organic chemistry.

Uploaded by

keenallan08
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© © All Rights Reserved
We take content rights seriously. If you suspect this is your content, claim it here.
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DRUG SYNTHESIS

Alkanes

They have the general formula CnH2n+2

CnH2n H2 Pt/Pd/Ni CnH2n+2 for example CH=CH C2H6


Ethene ethane
Alkane derivatives
Alkenes

They have the general formula CnH2n.

Their industrial source is by cracking of petroleum products.

(HMW)Alkanes metal catalyst H2 + smaller alkanes + alkenes

400-600oC
Alkene synthesis ;Dehalogenation of alkyl
halides
• Dehydration of alcohols by acids
Reactions of alkenes Betamethasone
Halohydrin formation
Alcohols
Side products of fermentation
Other methods of synthesis alcohols
Grignard synthesis from carbonyl compounds

+ C OMgX
RMgX
C O
Grignard reagent
R

H2O

+
Mg(OH)x C OH

R
The alcohol obtained depends on the starting
carbonyl compound
Mannich reactions
Other metallic reagents
Methyl pentynol
Ethynodiol
Hydrolysis of alkyl halides
Reduction of carbonyl compounds
Adrenaline
Meprobamate
Glycols
Metabolism
Ethers

• ROR
• Anaesthetic Ether
Ethers
Side products
Side products
Poor Storage
..
Halogenated compounds
Nitroglycerine
Williamson Synthesis
Reaction of Ethers;Cleavage using acids
They have the following general formula

Synthesis
 From alkenes
 From halohydrins
Aldehydes
Formalin derivatives
Other methods of synthesis
 Oxidation of alcohols

The aldehyde is distilled as it is formed before it is oxidized further to carboxylic acid.


 Oxidation of alkenes
Ketones
Can be synthesized using a number of methods

 Oxidation of secondary alcohols


 Reaction between a nitrile and a Grignard reagent
Sodium Valproate
 Oxidation of primary alcohols

 Carbonation of Grignard reagents

Carbon dioxide is bubbled through a Grignard reagent in dry ether. A mineral acid is added and
the carboxylic acid is form.
 Hydrolysis of nitriles
The nitrile is refluxed with aqueous mineral acids to give an amide that further hydrolysis to give
a carboxylic acid.

PhCHCHCOOEt PhCHCHCOOEt NH4+


H+/H2O + + H2O
CN COOH
CN COOH

CO2
O

Ph N
Me MeNH2 PhCHCH2

COOH
O COOH

Phensuccimide
..
Phenobarbital
Carbonic acid derivatives
From phosgene
Acid chloride –monofunctional
Phosgen -bifunctional
AMINES Reductions of nitro compunds
Reaction of alkyl halides with ammonia or amines
Reduction of oximes
ELECTROPHILIC AROMATIC SUBSTITUTIONS
Nitration
Friedel’s Crafts method
Sulfonation
Kolbe reactions
Friedels crafts reaction
Protonation of a double bond
Protonation of alcohols or carbonyl groups
By decomposition of Diazo compounds
Mannich reaction
Carbanions
Claisen Condensation
Dieckmann condensation

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