UGI reaction is a Multi-Component Reaction - powerful tool in drug discovery!

1. Ugi reactionUgi reaction

2. Ugi reaction is a Multi-Component
Reaction

3. A powerful tool
in Drug Discovery

4. Prof. Ivar Karl Ugi first
reported this
reaction in 1959.

5. What is Ugi reaction?
A Multi-Component Reaction [MCR]
between a ketone or aldehyde,
an amine, an isocyanide and a
carboxylic acid to form a
bis-amide.

6. Example
-H2O
Ketone
or AldehydeCarboxylic
acid
Amine Isocyanide
Bis-amide

7. Ugi reaction
 The Ugi reaction is exothermic!
 Usually completes in minutes
after isocyanide addition.
 This is an uncatalyzed reaction.
 Has high atom economy as only
a molecule of water is lost.
 High chemical yield.

8. Possible Mechanism
α-aminoacyl amide derivative

9. α-aminoacyl amide derivatives
OR
bis-amide
Changing substituents, R1, R2, R3, R4 and R5
a huge chemical Libraries can be built!
The Final Product...

10. Synthesis of complexHeterocyclic fused
rings

11. As a synthetic strategy, suitable selection of Starting
components can generate huge Chemical Libraries!

12. UGI Reaction provides Medicinal
Chemists with a powerful tool to
create Novel Chemical Diversity,
matching the space of Biological
Targets with relevant chemistry.
Application

13. Ugi Product
Diels-Alder
Ugi–Diels–Alder Product
Ugi–Diels–Alder reaction

14. MCRs have been used to create
diverse Combinatorial Libraries,
to accomplish the synthesis of
highly Complex Natural
Products as well as large-scale
production of drug candidates.
Application

15. Ugi–Heckreaction

16. This reaction is thus very
important for generating
Compound Libraries for
Screening purposes.

17. Ugi–Buchwald–Hartwig reaction

18. The discovery of novel MCRs
has become an increasingly
active area of research, yielding
novel Chemical Scaffolds for
Drug Discovery efforts.

19. Nature Journal recently
published a Review on Multi-
Components Reactions.
https://www.nature.com/articles/s41467-018-03784-x
Published online: 12 April 2018

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