The course will focus on synthetic methods and strategies as well as retrosynthetic analysis of known drugs. A short introduction to the biological and pharmacological properties of the drugs will also be included. At the end of the course the students will be prepared to discuss various synthetic routes and perform retrosynthetic analysis of common drugs for industrial production.

More in details:

• Refresh and update your knowledge of synthetic organic methods.
• Learn the latest on enantioselective reactions and catalytic organometallic reactions.
• Become familiar with the increasingly important applications of enzymes, catalytic antibodies, and other biological methods in organic chemistry.
• Gain an exposure to modern approaches for designing syntheses of complex organic compounds.
• See the applications of synthetic strategy and methods by means of numerous examples of actual syntheses taken from the original literature.
• Obtain an extensive compilation of references to the current synthetic organic chemistry literature right through the current year.

The course gives an introduction to the most common synthetic methods that are applied in industrial and laboratory drug synthesis. The course is a continuation of organic and medicinal chemistry taught during the first part of the pharmacy studies.

“The top reactions for medicinal chemistry”

The organic reactions that underpin contemporary medicinal chemistry will be discussed in details. For example, the course will cover amide bond formation, metal-catalyzed cross-couplings, heterocycle synthesis and modification.

More in details:

1. Scientific Computing Skills (Organic Chemistry software/database available free or on campus)
2. Reactions Used in the Pursuit of Drug Candidates
3. Applications of Transition Metal Catalysis in Drug Discovery And Development-
4. Embedding sustainability into reagent and solvent selection. Examples from Organic Process Chemistry- The Emergence of Base Metal Catalysis in Pharma
5. Masterpieces in Process Chemistry
6. An overview of the key routes to the best selling 5- and 6-membered ring nitrogen heterocyclic pharmaceuticals
7. The synthesis of active pharmaceutical ingredients (APIs) using continuous flow chemistry- The Synthesis Machine
8. Industrial natural product chemistry for drug discovery and development. Examples from Chemical Neuroscience.

The course is primarily open to students who have been admitted to the School of Pharmacy at the University of Urbino. If there is space available then others may also apply to take the course as long as their academic background is adequate.

Chemists who are involved in any aspect of laboratory or manufacturing operations concerned with the preparation of organic compounds and who wish to acquire a stronger background in the modern methods of organic synthesis and the strategies by which syntheses of organic compounds may be designed.

D1 – KNOWLEDGE AND UNDERSTANDING
At the end of this activity, students should be able to:
1) know the main aspects of stereochemistry and the methods used for determining the excesses of stereoisomers;
2) know the implications that connect the chirality with biological activity of a given molecules;
3) know the main sources of chiral molecules;
4) know the main aspects and peculiarities associated with fermentation and enzymatic processes;
5) know the main aspects and peculiarities associated with asymmetric synthesis;
6) Know the industrial approach for synthesizing specific molecules having industrial importance.

D2 – APPLYING KNOWLEDGE AND UNDERSTANDING
At the end of this activity, students should be able to:
1) classify molecules in terms of their stereochemistry;
2 identify the diastereomeric and enantiomeric excesses for a given mixture;
3 describe the main sources of chiral molecules;
4) describe the peculiarity of fermentation, enzymatic and asymmetric processes;
5) describe the industrial synthetic approach of molecules having industrial importance;

D3 – MAKING JUDGEMENTS
At the end of this activity, students should be able to:
1) propose the best technology to determine the stereoisomeric excess of a given mixture of stereoisomers on the basis of their structure;
2) compare the fermentation, enzymatic and asymmetric processes on the base of their respective advantages and disadvantages;
3) compare and evaluate the different synthesis approaches of molecules with proven industrial importance;

D4 – COMMUNICATION SKILLS
After completing the course, students will have to prove that they are able to clearly describe (in English) the use of various technologies and concepts learned during lessons.

D5 – LEARNING SKILLS
At the end of the activity, students should be able to find and apply new information, than those provided in the training activity, to evaluate and compare the different industrial synthetic approaches of molecules of industrial interest.

The teaching material prepared by the lecturer in addition to recommended textbooks (such as for instance slides, lecture notes, exercises, bibliography) and communications from the lecturer specific to the course can be found inside the Moodle platform › blended.uniurb.it

Lectures, seminars, and self-study.

In addtion, each student is required to read a number of review articles covering the following topics: Metathesis-reactions, Pd-catalysed reactions and enantio selective synthetic methods.

Teaching

Benefits

 

 
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• Current knowledge of organic synthesis

 
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• Familiarity with new concepts and strategies for organic synthesis

 
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• Introduction to new reactions and catalysts

 
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• Overview of current total synthesis

 
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• New directions in organic synthesis

 
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Attendance

Inactivity and / or excessive absences in compulsory education means that the student does not receive final assessment / examination

Course books

Contemporary Drug Synthesis, Jie-Jack Li, Douglas S. Johnson, Drago R. Sliskovic, Bruce R. Roth (Wiley-Interscience)

The Art of Drug Synthesis

Assessment

A one hour written exam followed with an oral individual examination for 30 minutes.

Disabilità e DSA

Le studentesse e gli studenti che hanno registrato la certificazione di disabilità o la certificazione di DSA presso l'Ufficio Inclusione e diritto allo studio, possono chiedere di utilizzare le mappe concettuali (per parole chiave) durante la prova di esame.

A tal fine, è necessario inviare le mappe, due settimane prima dell’appello di esame, alla o al docente del corso, che ne verificherà la coerenza con le indicazioni delle linee guida di ateneo e potrà chiederne la modifica.