Synthesis of Drug Substances 1200-1CHMSLEW6
The lecture covers the basics of medical chemistry and presents, in the form of a multimedia presentation, the specificity of pharmaceutical substances in comparison to other chemical substances. It explains the basic linear strategy and shows why a more advanced convergent strategy is preferred in the synthesis of pharmaceutical substances. The lecture presents what this strategy is all about and what are its basic advantages over other synthetic strategies. It also presents the difference between discovery synthesis and process synthesis. The lecture will present the basic motivations and principles of creating intellectual property protection in the field of synthesis of pharmaceutical substances. Selected issues related to the diagnosis of polymorphism in pharmaceutical substances and the basic methods of identifying and producing polymorphic forms will be presented. Methods of synthesizing sulfonamides from various starting structural fragments will be presented. Synthetic methods of pharmaceutical 1,3,5- and 1,2,4-triazines will be shown. Methods of synthesizing pharmaceutical substances from the group of benzothiazoles and tetrahydrobenzothiazoles will be presented. An exemplary convergent strategy for the synthesis of pharmaceutical substances will be shown. Some modern methods used in the synthesis of pharmaceutical substances will be discussed. All the material required for the written examination, mainly based on publications and patents, will be presented in lectures and made available to participants in the form of a set of slides.
Estimated student workload during the semester – 38 hours, including:
participation in classes – 15 hours
individual study after each lecture – 5 hours
exam preparation – 13 hours
consultations with the instructor – 5 hours
Main fields of studies for MISMaP
Type of course
Mode
Prerequisites (description)
Course coordinators
Learning outcomes
It is expected that the main effect of the teaching is that the participant of the lecture acquires the ability to present the essential elements of the strategy for the synthesis of pharmaceutical substances and the key steps of synthesis of selected classes of pharmaceutical substances. Participants of the lecture will gain the ability to describe the specific properties of pharmaceutical substances, distinguishing them from other chemical substances, and the ability to present the basic methods of studying their polymorphism. The teaching will also result in the participants learning the basic principles of creating patent protection for pharmaceutical substances and methods of their synthesis.
Knowledge: the graduate knows and understands:
K_W08 – to an advanced extent, the classification of organic compounds into classes corresponding to types of functional groups (nomenclature, structure, chemical reactions, methods of preparation, occurrence, and applications). The graduate knows and understands the mechanisms of selected organic reactions and their stereochemical aspects.
K_W12 – to an advanced extent, the methods and techniques for the synthesis and identification of organic compounds (with particular emphasis on pharmacologically important and biologically active compounds), using chemical, chromatographic, spectroscopic, and diffraction techniques.
K_W17 – to an advanced extent, the aspects of drug structure, action, and synthesis, and understands the interdisciplinary nature of designing new drugs and drug delivery systems. The graduate knows the basics of molecular modeling.
Assessment criteria
On-line written exam with video option, only from the material presented during the lecture. The exam contains a set of 15 questions to be answered in 1.5 hours. The set is sent during the examination to the lecture participant's university mailbox. After finishing the exam, the participant sends the answers back to the lecturer.
Practical placement
Work placements are not planned.
Bibliography
1. G. Patrick, Medicinal chemistry (Chemia medyczna, Pol.), PWN 2019.
2. A. Zejc, M. Gorczyca, Drug chemistry (Chemia leków, Pol.), PZWL 2008
Additional information
Additional information (registration calendar, class conductors, localization and schedules of classes), might be available in the USOSweb system: