Subjects

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Technology of Synthetic Drugs - GF243

Title:	Technologie syntetických léčiv
Guaranteed by:	Department of Pharmaceutical Chemistry and Pharmaceutical Analysis (16-16190)
Faculty:	Faculty of Pharmacy in Hradec Králové
Actual:	from 2023
Semester:	summer
Points:	0
E-Credits:	3
Examination process:	summer s.:written
Hours per week, examination:	summer s.:28/14, C+Ex [HS]
Capacity:	unlimited / 45 (40)
Min. number of students:	unlimited
4EU+:	no
Virtual mobility / capacity:	no
Key competences:
State of the course:	taught
Language:	Czech
Teaching methods:	full-time
Level:
Explanation:	(F 3.r.)
Note:	deregister from the exam date if a requisite was not fulfilled course can be enrolled in outside the study plan enabled for web enrollment

Guarantor:	prof. PharmDr. Martin Doležal, Ph.D.
Co-requisite :	GF299
In complex pre-requisite:	GF1002

Annotation -

The lectures and practical training follow the subjects of Organic Chemistry II, Pharmaceutical Chemistry I and II. The students get acquainted with the theory and methodology of chemical processes which are important for the drug large-scale production.

Last update: Doležal Martin, prof. PharmDr., Ph.D. (04.12.2025)

Course completion requirements -

...

Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)

Literature -

Obligatory:

. . In Doležal, Martin. Technologie syntetických léčiv . Praha: Univerzita Karlova - Karolinum, 1999, s. -. ISBN 80-7184-984-7..

Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)

Teaching methods -

The training in Technology of Synthetic Drugs runs in 6th semester of pharmacy course in lectures, practical training and tutorials. The subject is finished by an exam.

Last update: Doležal Martin, prof. PharmDr., Ph.D. (18.02.2025)

Syllabus -

Lectures

Introduction
History and development of the pharmaceutical industry, Good Manufacturing Practice, Technical documents in pharmaceutical industry - quality control system
Chemical processes used in the syntheses of drugs:
General reactions for:
? Oxidation (Oxidation of hydrocarbons, Oxidation of aromatic system, Oppenauer Oxidation)
? Reduction (Catalytic Hydrogenation, Béchamp Reduction, Clemmensen Reduction, Wolff-Kishner Reduction, Meerwein-Ponndorf-Verley Reduction)
? Condensation (Aldol Condensation, Perkin Reaction, Claisen-Smidt Condensation, Knoevenagel Condensation, Claisen Condensation, Dieckmann Reaction, Mannich Reaction)
? Addition (Addition on bond carbon-carbon, Diels-Alder Reaction, Michael Reaction, Addition on bonds carbon-oxygen and carbon-nitrogen)
? Polymeration and polycondensation
? Isomerization and rearrangement (Wagner-Meerwein Rearrangement, Wolff Rearrangement, Arndt-Eistert Synthesis, Benzilic Acid Rearrangement, Hofmann Reaction, Curtius Rearrangement, Schmidt Reaction)
Special synthetic reactions for:
? Preparation of bond carbon-carbon (Friedel-Crafts Reaction, Gattermann Aldehyde Synthesis, Houben-Hoesch Reaction, Knorr Pyrazole Synthesis, Grignard Reaction, Reformatskii Reaction, Wurtz-Fittig Reaction, Blanc (Chloromethylation) Reaction)
? Preparation of bond carbon-hydrogen (Dehalogenation, Dehydroxylation, Deamination, Decarbonylation, Decarboxylation, Desulfonylation)
? Preparation of bond carbon-halogen (Halogenation, Finkelstein Reaction, Sandmeyer Reaction, Gattermann Reaction)
? Preparation of bond carbon-oxygen (Williamson Synthesis)
? Preparation of bond carbon-nitrogen
? Preparation of bond carbon-sulfur

Practical Training
Syntheses of representative types of drugs (Sulfanilamides, Benzocain, Clofibrat, Disulfiram, Etophyllin etc.). Excursion in a pharmaceutical manufacturing company.

Last update: Doležal Martin, prof. PharmDr., Ph.D. (07.02.2022)

Learning outcomes -

The Synthetic Drug Technology course builds on the successful completion of Organic Chemistry II and Pharmaceutical Chemistry. Students will gain basic knowledge and an overview of the history and development of API production, the emergence of the pharmaceutical industry, and the importance of Good Manufacturing Practice. They will be able to classify and, where appropriate, use basic technical documentation in the pharmaceutical industry.

They will gain basic theoretical and practical knowledge of the application of chemical processes used in laboratory preparation, pilot plant, and industrial production of drugs. They will learn how to use microwave technology and preparative chromatography in practice.

Using examples of the synthesis of selected chemical drugs, they will be able to describe general reactions such as oxidation, reduction, condensation, addition, polymerization, polycondensation, isomerization, and rearrangement.

Students will be well versed in and, using examples of the synthesis of selected drugs, will demonstrate special synthetic reactions in which new C-C, C-H, C-X, C-O, C-N, and C-S bonds are formed.

Practical exercises will focus on multistep syntheses of selected drugs. The course also includes an excursion to a pharmaceutical company focused on the development and production of API.

Last update: Doležal Martin, prof. PharmDr., Ph.D. (04.12.2025)