SFAB20039U Cancelled Design, Synthesis and Reactivity in Medicinal and Biopharmaceutical Chemistry
BSc Programme in Pharmacy - elective
The course will focus on how drug molecules are designed and synthesized - from a chemical perspective. Thus, different ways of accessing pharmaceutically relevant compound classes will be investigated. Strategic considerations with respect the order of introduction of functional groups and linear/convergent approaches will be discussed and compared.
The course will be organized around specific reaction types and functional groups where the most efficient way of accessing these will be highlighted. Furthermore, consideration about the metabolic liability and possible biotransformation of different functional group will be covered to guide the design process of new drug molecules.
Specific themes that will be covered include:
- Synthesis of drugs using state-of-the-art methodologies - Enantioselective synthesis, cross coupling ractions, C-H activation, etc.
- Reactive functional groups in medicinal chemistry
- Bioorthogonal chemistry
- Biopharmaceuticals
Lectures on lead optimization and process development within the pharmaceutical industry will be given by researchers from the industry
At the end of the course, students are expected to be able to:
Knowledge
- identify the functional groups typically encountered in drug discovery and process development and reflect upon their reactivity and stability
- explain basic elements of selected reaction mechanisms, such as cross-coupling reactions
- summarize and critically evaluate strategies in modern organic synthesis as applied in lead optimization and process development cases in medicinal and biopharmaceutical chemistry
- describe and discuss different types metabolic reactions, the reaction mechanism and propose typical reactive hot-spots as well as expected metabolites
Skills
- master retro-synthetic strategies presented during the course
- analyze and evaluate the use of protection groups in synthesis planning
- assess and discuss biotransformation of functional groups in relation to selected drug discovery projects
- critically review and present examples from the scientific literature
Competencies
- design new drug candidates ligands where consideration about reactivity and metabolic liability are implemented
- plan and discuss synthetic strategies for putative drug molecules relevant for early discovery
Reviews and original scientific papers will be available at the course homepage
Further recommended reading: Jonathan Clayden, Nick Geeves, Stuart Warren (2012) Organic Chemistry 2nd Edition; ISBN: 978-0199270293 Oxford University Press
To each theme, the students will have access to 6-8 multiple choice questions in Absalon. These questions are formulated in such a way that the students can solve them if they have read, worked with and understood the curriculum of the day. The Quizz with close as the lectures start and the Quizz Report will be evaluated and discussed in plenum with the students. The intention of these Assignment Quizzes is multifold:
1) To ensure the students work with the curriculum before attending the lectures
2) Reward and encourage the students professionally
3) Improve the student learning
4) Provide a live picture of the actual skill level and identify ‘easy’ and ‘difficult’ subjects.
The Quizz will be accompanied with more elaborate explanations for correct answers and help/guidelines for false answers. The Quizz will also be opened again as the students start preparing for the exams.
Furthermore, the course teachers will provide an overview lecture with focus and key learning elements in the subjects of the day. Each lecture will terminate with a summary of the major skills and competences acquired.
In addition, the course will also use classical problem solving and exercises in the classroom. They serve both as student activating initiatives and to break up lectures in pieces no longer than 20 minutes.
- Category
- Hours
- Lectures
- 24
- Preparation
- 125
- Exercises
- 40
- Exam Preparation
- 16
- Exam
- 1
- Total
- 206
This course is not available for credit transfer students and other external students.
- Credit
- 7,5 ECTS
- Type of assessment
- Practical oral examination, 30 minContinuous assessment
- Type of assessment details
- For the final assessment, students are divided into groups of
three-four students.
Each group will receive a scientific paper and then have 48 hours to prepare a presentation in the form of powerpoint slides or a poster. The task will be to analyze, critically review and present the paper. Each student will have an individual assessment based on the presentation submitted by the group (max 10 min) followed by a discussion (max 10 min). - Aid
- All aids allowed
- Marking scale
- passed/not passed
- Censorship form
- No external censorship
Criteria for exam assesment
To pass the course the student must be able to:
Knowledge
- identify the functional groups typically encountered in drug discovery and process development and reflect upon their reactivity and stability
- explain basic elements of selected reaction mechanisms, such as cross-coupling reactions
- summarize and critically evaluate strategies in modern organic synthesis as applied in lead optimization and process development cases in medicinal and biopharmaceutical chemistry
- describe and discuss different types metabolic reactions, the reaction mechanism and propose typical reactive hot-spots as well as expected metabolites
Skills
- master retro-synthetic strategies presented during the course
- analyze and evaluate the use of protection groups in synthesis planning
- assess and discuss biotransformation of functional groups in relation to selected drug discovery projects
- critically review and present examples from the scientific literature
Competencies
- design new drug candidates ligands where consideration about reactivity and metabolic liability are implemented
- plan and discuss synthetic strategies for putative drug molecules relevant for early discovery
Course information
- Language
- English
- Course code
- SFAB20039U
- Credit
- 7,5 ECTS
- Level
- Bachelor
- Duration
- 1 block
- Placement
- Block 3
- Schedule
- A
- Course capacity
- 70 students - 60 seats reserved for bachelor students
Study board
- Study Board of Pharmaceutical Sciences
Contracting department
- Department of Drug Design and Pharmacology
Contracting faculty
- Faculty of Health and Medical Sciences
Course Coordinators
- Jesper Langgaard Kristensen (17-706b79766b783471786f797a6b74796b7446797b746a34717b346a71)
Lecturers
Jesper Langgaard Kristensen and John Nielsen