Drug design and discovery - AP110025
Title: Drug design and discovery
Guaranteed by: Department of Organic Chemistry (110)
Faculty: Faculty of Chemical Technology
Actual: from 2023
Semester: summer
Points: summer s.:0
E-Credits: summer s.:0
Examination process: summer s.:
Hours per week, examination: summer s.:2/0, other [HT]
Capacity: unknown / unknown (unknown)
Min. number of students: unlimited
State of the course: taught
Language: English
Teaching methods: full-time
Teaching methods: full-time
Level:  
Note: course is intended for doctoral students only
can be fulfilled in the future
Guarantor: Brancale Andrea prof. Ph.D.
Examination dates   
Annotation
Synthetic strategies based on organocatalyzed processes, such as stereoselective aldol and Mannich reaction, Michael and Diels-Alder addition, Friedel-Crafts-like functionalization, allylation, transfer hydrogenation, and hydrosilylation, etc.
Last update: Fialová Jana (05.05.2022)
Aim of the course -

Students will be able to:

perceive organocatalytic reactions in terms known to you from the previous courses on organic chemistry and biochemistry

recognise and understand the basic organocatalytic reactions

understand the mechanisms of organocatalyzed reactions and to broaden the mechanistic understanding in general organic chemistry.

identify conditions required for catalytic cycles to be efficient.

use organocatalysis for designing key steps in the synthesis of organic molecules.

Last update: Fialová Jana (05.05.2022)
Course completion requirements -

It is compulsory to pass written examination test.

Last update: Fialová Jana (05.05.2022)
Literature -

R: P. I. Dalko (Ed.): Enantioselective Organocatalysis - Reactions and Experimental Procedures; Wiley-VCH, Weinheim, 2007.

A: P. I. Dalko (Ed.): Comprehensive Enantioselective Organocatalysis - Catalysts, Reactions, and Applications, Vol. 1-3; Wiley-VCH, Weinheim, 2013.

A: R. Rios-Torres (Ed.): Stereoselective Organocatalysis; Wiley, Hoboken, USA, 2013

Last update: Fialová Jana (05.05.2022)
Syllabus

1. Introduction.

2. Catalysis via Enamines; Aldol reactions, Mannich reactions,α-Heteroatom Functionalization, Michael Additions.

3. Catalysis via Iminium Ions; Cycloadditions, Michael additions, Epoxidations.

4. Brønsted Acids as Catalysts; Michael addition, Hydrocyanation, Mannich reaction, Aza-Henry reaction, Aza-Friedel-Crafts reaction, Pictet-Spengler Reaction, Transfer Hydrogenation, Morita-Baylis-Hillman Reaction, Diels-Alder Reaction.

5. Lewis Bases as Catalysts; Allylation of Aldehydes, Aldol-Type Reactions, Hydrocyanation, Hydrosilylation, Reduction of Imines, Reduction of Ketones.

6. Epoxidation.

Last update: Fialová Jana (05.05.2022)
Learning resources -

http://en.wikipedia.org/wiki/Organocatalysis

Last update: Fialová Jana (05.05.2022)