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Schmidt Reaction

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What is Schmidt Reaction? 

The Schmidt reaction is an important name reaction of organic chemistry. In this reaction azide (conjugate base of hydrazoic acid) reacts with a carbonyl derivative (such as carboxylic acid, aldehyde, ketone) under acidic conditions to give amine or amides with release of nitrogen. It is a rearrangement reaction. That’s why it is also known as Schmidt rearrangement reaction. This reaction is very closely reacted to another name reaction called Curtius rearrangement. 

When Schmidt reaction takes place with carboxylic acid, it gives amine while when it takes place with ketone, it gives amides. Although in Schmidt reactions of both carboxylic acid and ketone, hydrazoic acid is used and nitrogen gets released. 

Schmidt Reaction with Carboxylic Acid –

Carboxylic acid + Hydrazoic acid 🡪 Primary amine + Carbon dioxide + Nitrogen 

Reaction –

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Schmidt Reaction with Ketone –

Ketone + Hydrazoic acid 🡪 Amide + Nitrogen 

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Schmidt reaction is named after Karl Friedrich Schmidt (1887 - 1971). As Karl Friedrich Schmidt 1st reported the reaction by converting benzophenone and hydrazoic acid to benzanilide in 1924. Although Schmidt reaction for carboxylic acid was not reported until 1991. 

Mechanism of Schmidt Reaction 

First, we are describing here the mechanism of Schmidt reaction with carboxylic acids. Mechanism of this reaction can be understood by following 5 steps –

Step 1. Formation of Acylium Ion – Schmidt reaction with carboxylic acid starts with formation of acylium ion. It is formed by protonation of carboxylic acid with removal of water molecule. Reaction is given below –

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Step 2. Acylium Ion Reaction with Hydrazoic Acid – Acylium ion reacts with hydrazoic acid and forms protonated azido ketone. Reaction is given below –

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Step 3. Rearrangement of Azido Ketone – Now azido ketone undergoes rearrangement with alkyl group (R) migrating over the C-N bond and with removal of nitrogen gas. Rearrangement of azido ketone forms protonated isocyanate. Reaction is given below –

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Step 4. Formation of Carbamate – Water molecule attacks on the protonated isocyanate and forms carbamate. Reaction is given below –

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Step 5. Deprotonation of Carbamate and Formation of Amine – Now carbamate undergoes deprotonation and forms carbon dioxide and amine. Reaction is given below –

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Mechanism of Schmidt Reaction of Ketones 

Mechanism of Schmidt reaction of ketone can be understood by following steps through Beckmann rearrangement –

Step 1. Activation of Carbonyl Group of Ketone – The carbonyl group of ketone is activated by protonation for nucleophilic addition by the azide. Reaction is given below -

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Step 2. Formation of Azidohydrin – Azidohydrin is formed by nucleophilic addition of nucleophile N3- at activated carbon of carbonyl group of ketone. Reaction is given below –

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Step 3. Formation of Diazoiminium – Azidohydrin loses water molecules in an elimination reaction to give diazoiminium. Reaction is given below –

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Step 4. Formation of Nitrilium Intermediate – One of the alkyl (or aryl) groups migrates from carbon of diazoiminium to nitrogen with loss of nitrogen to give a nitrilium intermediate as in the Beckmann rearrangement. Reaction is given below –

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Step 5. Formation of Imidic Acid – Now a water molecule attacks on nitrilium intermediate and converts it into protonated imidic acid. 

Step 6. Formation of Amide – Now imidic acid undergoes loss of proton to arrive at its tautomer of the final amide. Reactions of step 5 and 6 are given below together –

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In an alternative mechanism, reaction may occur in a similar manner as Baeyer – Villiger reaction to give protonated amide. 

Schmidt Reaction and Curtius Rearrangement 

Schmidt reaction and Curtius rearrangement are closely related reactions. In Curtius rearrangement reaction acyl azide is produced by the reaction of acid chloride with sodium azide and the acid chloride is formed by the reaction of carboxylic acid with SOCl2 . While in Schmidt reaction acyl azide is produced by reaction of the carboxylic acid with hydrazoic acid as discussed under the section – What is Schmidt Reaction?

For your better understanding we are giving here a brief explanation of Curtius rearrangement. 

Curtius Rearrangement - Theodor Curtius was doing various experiments with acyl azides. During these experiments he discovered that on thermal decomposition of an acyl azide, it gives isocyanate with loss of nitrogen gas. The isocyanate on reaction with alcohols gives carbamate and with water and amines gives primary amine and urea derivatives respectively. The reaction is given below –

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Thus, Curtius rearrangement reaction is thermal decomposition of carboxylic azides (such as acyl azide) to give isocyanate. In Curtius rearrangement acyl azide can be prepared by either reaction of acid chlorides or acid anhydrides with sodium azide or trimethyl azide or direct reaction of carboxylic acid with diphenylphosphoryl azide. Reactions are given below –

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This ends our coverage on the topic “Schmidt Reaction”. We hope you enjoyed learning and were able to grasp the concepts. We hope after reading this article you will be able to solve problems based on the topic and will not get confused between Curtius Rearrangement and Schmidt Reaction. If you are looking for solutions to NCERT Textbook problems based on this topic, then log on to Vedantu website or download Vedantu Learning App. By doing so, you will be able to access free PDFs of NCERT Solutions as well as Revision notes, Mock Tests and much more. 

FAQs on Schmidt Reaction

1. What is the Schmidt reaction?

The Schmidt reaction is an organic reaction where an azide, specifically hydrazoic acid (HN₃), reacts with a carbonyl derivative, such as a carboxylic acid, ketone, or aldehyde, in the presence of a strong acid catalyst (like concentrated H₂SO₄). This reaction is primarily used for synthesising amines from carboxylic acids and amides from ketones.

2. What are the essential reagents used in the Schmidt reaction?

The key reagents required for the Schmidt reaction are:

  • Substrate: A carbonyl-containing compound like a carboxylic acid or a ketone.
  • Azide Source: Hydrazoic acid (HN₃), which is highly toxic and explosive, often generated in situ from sodium azide (NaN₃) and a strong acid.
  • Catalyst: A strong protic acid, most commonly concentrated sulfuric acid (H₂SO₄), which protonates the carbonyl group and facilitates the reaction.

3. How can you prepare a primary amine from a carboxylic acid using the Schmidt reaction?

To prepare a primary amine from a carboxylic acid (RCOOH) using the Schmidt reaction, the carboxylic acid is treated with hydrazoic acid (HN₃) in the presence of concentrated sulfuric acid. The reaction proceeds through an acyl azide and an isocyanate intermediate (R-N=C=O), which then hydrolyses to yield a primary amine (RNH₂) with one less carbon atom than the parent carboxylic acid, along with the evolution of carbon dioxide gas.

4. What is the product when a ketone reacts in the Schmidt reaction?

When a ketone (RCOR') reacts with hydrazoic acid under acidic conditions, it undergoes the Schmidt reaction to form a substituted amide. The reaction involves the insertion of a nitrogen atom between the carbonyl carbon and one of the alkyl/aryl groups. For example, reacting acetone (CH₃COCH₃) yields N-methylacetamide (CH₃CONHCH₃).

5. What is the step-by-step mechanism of the Schmidt reaction with a carboxylic acid?

The mechanism for the reaction of a carboxylic acid involves several key steps:

  • Step 1: The carboxylic acid is protonated by the strong acid catalyst to form a protonated carbonyl group.
  • Step 2: Hydrazoic acid (HN₃) acts as a nucleophile and attacks the carbonyl carbon, followed by dehydration to form an acyl azide intermediate.
  • Step 3: The acyl azide loses nitrogen gas (N₂) to form an acylnitrene, which immediately rearranges. The alkyl/aryl group (R) migrates from the carbonyl carbon to the nitrogen atom, forming an isocyanate intermediate (R-N=C=O).
  • Step 4: The isocyanate is then hydrolysed by water to form a carbamic acid, which is unstable and decarboxylates (loses CO₂) to give the final primary amine (RNH₂).

6. How does the Schmidt reaction differ from the Hofmann and Curtius rearrangements?

While all three reactions can produce primary amines, they differ in their starting materials and reagents.

  • Schmidt Reaction: Starts with a carboxylic acid and uses hydrazoic acid (HN₃) and H₂SO₄.
  • Hofmann Rearrangement: Starts with a primary amide (RCONH₂) and uses bromine (Br₂) or chlorine (Cl₂) in an aqueous solution of sodium hydroxide (NaOH).
  • Curtius Rearrangement: Starts with an acyl azide (RCON₃), which is typically prepared from an acyl chloride, and undergoes thermal or photochemical decomposition.
All three proceed through a common isocyanate intermediate.

7. In the Schmidt reaction with an unsymmetrical ketone, what determines which group migrates?

In the Schmidt reaction of an unsymmetrical ketone (RCOR'), the choice of which group (R or R') migrates to the nitrogen atom is determined by migratory aptitude. The group that is bulkier and/or can better stabilise a positive charge will preferentially migrate. The general order of migratory aptitude is: Tertiary alkyl > Cyclohexyl > Secondary alkyl > Aryl (phenyl) > Primary alkyl > Methyl. The group with the higher aptitude migrates, influencing the structure of the resulting amide.

8. What are some important applications of the Schmidt reaction in organic synthesis?

The Schmidt reaction is a versatile tool in organic chemistry with several key applications beyond simple amine synthesis. It is used in:

  • The synthesis of complex natural products and pharmaceuticals containing amine or amide functional groups.
  • The creation of α-amino acids from β-keto esters.
  • Ring expansion reactions, for instance, converting a cyclic ketone like cyclohexanone into a seven-membered cyclic amide (a lactam) called caprolactam, which is a monomer for Nylon 6.
  • The synthesis of substituted anilines from benzoic acids, which are important precursors in the dye and drug industries.