Synthesis and technology of active compounds 0600-S1-CM-STSA

Lecture:
Physicochemical foundations of technological processes. Technological principles. Technological diagrams. Raw Materials. Tasks of chemical technology, selection of conditions for conducting a technological process and its division into unit activities (unit operations, unit processes). Principles of rational use of raw materials and energy. Green Chemistry. Pharmaceutical industry in Poland. Methods used in the broadly understood "drug discovery". Methods for selecting a candidate for a therapeutic agent, as well as methods for its synthesis and isolation in laboratory and industrial conditions. Selection of reagents and solvents taking into account the requirements for product purity and environmental protection. The selected examples will show the optimization of the synthesis pathways of active agents and the analytical methods necessary in the quality control process of the final product. Methods for the preparation and resolution of optically active compounds by resolution of racemic mixtures. Stereoselective synthesis.
Laboratory:
During the laboratory exercises, students perform selected unit operations used in the technology of active substances: extraction, distillation, crystallization, evaporation, filtration, drying.
They independently synthesize the basic active compounds used in pharmaceutical preparations and therapeutic agents. They determine their structure by spectroscopic methods and purity by chromatographic methods. Two-step synthesis of Propranolol. Aspirin synthesis. Paracetamol synthesis. Cardiamid synthesis. Urotropin synthesis.

Total student workload

1. 20h lecture, 70h laboratory, 25h consultation, i.e. 115 contact hours, 2. 30 hours individual work, 3. 30h time required to prepare in the assessment process, 175h / 25 = 7ECTS

Learning outcomes - knowledge

W1: has knowledge of thc issues of chemical technology, processes and unit operationr - K_W01 W2: knows the methods of producing selected active substances and auxiliary substances, used physical operations and unit chemical processes - K_W07 W3: knows the analytical methods used in the control of technological processes - K_W04 W4: knows the methods of organic chemistry in the synthesis of new active substances - K_W07 W5: knows the methods of seeking new medicinal substances and the use of combinatorial chemistry in the synthesis of active substances - K_W04 W6: knows the role of medical chemistry in the drug discovery process - K_W11

Learning outcomes - skills

U1: can describe ecological technologies, can indicate the criteria of nuisance of traditional technologies, solve problems related to the implementation of technological processes - K_U01 U2: can choose the conditions for the production of active substances based on basic physical operations and chemical processes - K_U01, K_U06 U3: can perform simple operations and unit processes - K_U04 U4: selects the right substrates for synthesis, can recover and utilize them - K_U06

Learning outcomes - social competencies

K1: knows the limitations of own knowledge in the field of synthesis and technology of active substances understands the need for further education and improvement of professional competence - K_K01 K2: can select information, draw conclusions - K_K03 K3: is aware of the responsibility for jointly implemented tasks related to teamwork - K_K07

Teaching methods

Lecture: Conventional, informative lecture using multimedia presentations - giving method Laboratory: Seeking teaching methods: conducting experiments alone to simulate selected processes, classical method

Expository teaching methods

- informative (conventional) lecture
- problem-based lecture

Exploratory teaching methods

- experimental
- laboratory
- practical
- classic problem-solving

Prerequisites

Basic knowledge of general chemistry, analytical chemistry, instrumental analysis

Course coordinators

Urszula Kiełkowska
Andrzej Wolan

Assessment criteria

Lecture: written exam (multiple choice and open questions) - W1-W6, U1, K1
Includes content presented in lectures
Laboratory: passing the grade - W2-W4, U2-U4, K1-K3
continuous assessment of the student during classes (participation in classes, commitment, diligence, preparation for classes)
students are required to pass an initial colloquium on health and safety at work and unit operations. During the laboratory, they also take a test on the synthesis and analysis of active substances. As part of the exercises, students perform selected unit operations and the synthesis of preparations (medicaments) prescribed by the assistant, present a report on the performed experiments together with a summary and discussion of the results.
Assessment criteria:
Final block assessment: 70% exam results + 30% lab results
The thresholds are assessed by the Nicolaus Copernicus University regulations
threshold required for satisfactory - 50-60%, satisfactory plus - 61-65%, good 66-75%, good plus 76-81%, very good - 82-100%
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Bibliography

Literature:
E. Bortel, H. Koneczny, Zarys technologii chemicznej, PWN, Warszawa 1992.
Praca zbiorowa, Technologia chemiczna nieorganiczna, WNT, Warszawa 1965.
Technologia nowoczesnych postaci leków, pod redakcją R.H. Mullera i G.E. Hildebrand, Wydawnictwo Lekarskie PZWL, Warszawa, 2003.
G. L. Patrick, Chemia medyczna, WNT, Warszawa, 2003.
T. Tkaczynski, D. Tkaczynska „Synteza i technologia chemiczna leków”, PZWL 1984.
A. I. Vogel ” Preparatyka organiczna” WNT, Warszawa 2009.
Literatura uzupełniająca:
R. E. Kirk-Othmer, Encyclopedia of Chemical Technology, John Wiley&Sons, New York 2007.
A. Zieliński, Technologia chemiczna organiczna, WNT, Warszawa 1973.
Douglas S. Johnson, Jie Jack Li, The Art of Drug Synthesis, Wiley, 2007
L. F. Tietze, T. Eicher, U. Diederchsen, A. Speicher, Reaction and Syntheses, Wiley, 2007.
P. Mastalerz, „Chemia organiczna” Wydawnictwo Chemiczne, Wrocław 2000

Additional information

Additional information (registration calendar, class conductors, localization and schedules of classes), might be available in the USOSweb system:

Description of 0600-S1-CM-STSA in USOSweb