Synthesis of Heterocyclic Compounds and Their Application in Therapy

Adatok

A Tantárgybejelentőben megadott hivatalos adatok az alábbi tanévre: 2020-2021

Tematika

Heterocyclic chemistry is an important subdivision of organic chemistry, as 70% of all medicines are heterocyclic compound or contains a heterocyclic moiety. This course will give an introduction to, and the summary of, the most important principles and ideas of heterocyclic chemistry. This course partially re-calls the knowledge of Organic chemisty 1 and Organic chemistry 2 course, discusses those details which were not reflected on, because of time shortage and supports to evaluate the pharmacological chemistry subject.
-Electronic structure of heterocycles
-Nomenclature of heterocyclic compounds
-Main synthetic routes to heterocyclic compounds, Saturated heterocycles, occurence of heterocycles
-Three and four membered heterocycles (synthesis, reactions, occurence)
-The pyrrole and indole (synthesis, reactions, occurence)
-Furan, thiophene and their benzo derivatives.
-Five membered heterocycles with two or more heteroatoms: imidazole, oxazole, thiazole
-Pyrazole, isoxazole, isothiazole
-I. st test, Six-membered heterocycles with one oxygen heteroatom (piranes, chromones, flavones and coumarins)
-Six membered heterocycles with one nitrogen atom (pyridine, quinoline, isoquinoline)
-Six membered heterocycles with two or more heteroatoms (purine, diazines, triazines etc.)
-Seven membered heterocyclic chemistry
-Heterocycles in supramolecular chemitry
-Heterocyclic compounds in organic snthesis
-II nd test, short presntation on a paper on heterocyclic chemistry
-Evaluation

Előadások

Gyakorlatok

Szemináriumok

• 1. Electronic structure of heterocycles, nomenclature of heterocycles
• 2. Occurence of heterocyclic compounds
• 3. Synthesis of heterocycles
• 4. Common reaction types in heterocyclic chemistry
• 5. Tautomerism in heterocyclic chemistry
• 6. Saturated heterocycles
• 7. Three and four membered heterocycles, beta lactams
• 8. Three and four-membered heterocycles and beta lactams
• 9. Synthesis of pyrroles and porfirine ring containing compounds
• 10. Synthesis of indoles, main reactions of indoles.
• 11. Furans and thiophenes
• 12. Thiophenes and benzothiophenes
• 13. 1,2-azoles, their synthesis, reactions and their occurence in drugs
• 14. 1,3-azoles, their synthesis, reactions, occurence in drugs
• 15. 1st test (generral feature of heterocyclic compounds (3-, 4-, 5-membered heterocycles)
• 16. Six membered heterocycles containing oxygen heteroatom
• 17. Pyridines (synthesis, reactions, occurence in drugs and biomolecules)
• 18. Quinolines, isoquinolines (synthesis, reactions, occurence in drugs)
• 19. Synthesis of pyrimidines and their occurence in medicines
• 20. Synthesis and reactions of 1,2- and 1,4-diazines
• 21. Synthesis and reactions of triazines and purines
• 22. Heterocycles of life and death
• 23. Seven membered heterocycles their occurence, synthesis, applications in therapy
• 24. IInd test, short presentations on papers on heterocyclic chemistry, evaluation
• 25. Heterocycles in supramolecular chemistry
• 26. Heterocycles in organic synthesis
• 27. 2nd test (6- and 7-membered heterocycles)
• 28. Short presentations, evaluations

A tananyag elsajátításához szükséges segédanyagok

Kötelező irodalom

Li, J. J. Hetrocyclic chemistry in Drug Discovery, Wiley

Saját oktatási anyag

Slides will be given to students as a ppt or pdf files.

Jegyzet

Joule, J. J.; Mills, K. Heterocyclic chemistry at a Glance. (Wiley)

Ajánlott irodalom

Li, J. J. Top 10 drugs Oxfors University Press

A félév elfogadásának feltételei

Maximum of 25 % absence allowed

Félévközi ellenőrzések

The students write two tests, at the middle of the semester and at the end of the semester. Every student have a chance to make a presentation based on a heterocyclic chemistry paper for an extra grade.

Távolmaradás pótlásának lehetőségei

Personal communication. The english program student might visit the paralell hungarian course to catch up the main reaction equations.

Vizsgakérdések

-Electronic structure of heterocycles
-Nomenclature of heterocyclic compounds
-Main synthetic routes to heterocyclic compounds
-Saturated heterocycles
-Three and four membered heterocycles (synthesis, reactions, occurence)
-The pyrrole and indole (synthesis, reactions, occurence)
-Furan, thiophene and their benzo derivatives.
-Five membered heterocycles with two or more heteroatoms
-Six-membered heterocycles with one oxygen heteroatom (piranes, chromones, flavones and coumarins)
-Six membered heterocycles with one nitrogen atom (pyridine, quinoline, isoquinoline)
-Six membered heterocycles with two or more heteroatoms (purine, diazines etc.)
-Seven membered heterocyclic chemistry
- Heterocycles in supramolecular chemitry
-Heterocyclic compounds in organic snthesis

Vizsgáztatók

Gyakorlatok, szemináriumok oktatói

• Dr. Kálai Tamás