Synthesis of Heterocyclic Compounds and Their Application in Therapy

Daten

Offizielle Daten in der Fachveröffentlichung für das folgende akademische Jahr: 2020-2021

Thematik

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

Vorlesungen

Praktika

Seminare

• 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

Materialien zum Aneignen des Lehrstoffes

Obligatorische Literatur

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

Vom Institut veröffentlichter Lehrstoff

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

Skript

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

Empfohlene Literatur

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

Voraussetzung zum Absolvieren des Semesters

Maximum of 25 % absence allowed

Semesteranforderungen

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.

Möglichkeiten zur Nachholung der Fehlzeiten

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

Prüfungsfragen

-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

Prüfer

Praktika, Seminarleiter/innen

• Dr. Kálai Tamás