Tailor-made Training Organic Synthesis in Early Drug Discovery

This course covers the most important principles and reactions in synthetic organic chemistry that are applied in the early stages of the drug discovery process. Topics such as nucleophilic and electrophilic substitution reactions, elimination and addition reaction mechanisms, and the chemistry of enolates and heterocycles are covered.

General

About the training

Through a combination of lectures, practicing with exercises and a written examination, you will learn to understand and apply the fundamental reactions that are essential for the synthesis of pharmaceutically active compounds.

During this course, you will learn about the general principles and fundamental reactions used in synthesis routes in the early stages of the drug discovery process, in particular:

Definitions, basic principles and nucleophilic additions to carbonyl compounds
Nucleophilic substitution to saturated carbons
Elimination reactions
Electrophilic addition to alkenes and electrophilic aromatic substitution
Basic principles of enolate chemistry
Reactions of enolates with carbonyl electrophiles
Addition to electrophilic alkenes; reactions with sulphur (S), phosphorus (P) and silicon (Si), oxidation/reduction
Heterocyclic chemistry, synthesis of functionalised aromatic heterocycles

What do former participants say about the training course?

I found it really nice to first have a recap of the information and then applying it with exercises.

- Participant in-company programme for Pivot Park

For whom is the training intended?

For professionals working in drug development, such as researchers or laboratory technicians: Candidates must have a bachelor's degree in one of the molecular sciences (chemistry, molecular life sciences, biology, physics) or a related field.

What does the training provide?

After successfully completing this course, you will understand the fundamental chemical reactions involved in the synthesis of pharmaceutically active compounds and be able to apply this knowledge.

Upon satisfactory attendance and passing the test, participants will receive a Microcredential worth 3 ECTS credits. This digital certificate is stored in the digital backpack and can be shared with colleagues or employers, for example via LinkedIn.

This course was developed with funding from ZonMW

This course was developed with funding from ZonMW (PharmaNL). The aim is to develop an Early Drug Discovery Education Track consisting of eight post-graduate courses that meet the wishes and needs of the business community. We are collaborating with HAN University of Applied Sciences on this project. This project strengthens the current range of pharmaceutical training courses with innovative Early Drug Discovery (EDD) lifelong learning courses. These are intended for employees of companies in the pharmaceutical sector at post-graduate and post-university level. More information can be found on the ZonMW website.

Starting date

To be announced

Main Language

English

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Factsheet

Type of education

Training

Organisation

Education for Professionals

Contact information

Do you have a question about this tailor-made training programme? Or are you curious about how we can develop a fully tailor-made programme for your organisation? If so, please contact us.

Programme

The Organic Synthesis in Early Drug Discovery course consists of a total of eight half-days spread over 16 weeks, and a final exam. A study guide is available, and the book Organic Chemistry (Clayden, Greeves and Warren, Oxford, second edition) is used. The course (and the test) will be conducted in English. Participants will have access to the study materials via the Brightspace digital learning environment. The following eight topics will be covered in the course:

Lecture 1: Definitions, basic principles, and nucleophilic additions to carbonyl compounds
Lecture 2: Nucleophilic Substitution at Saturated Carbons
Lecture 3: Elimination Reactions
Lecture 4: Electrophilic Addition to Alkenes and Electrophilic Aromatic Substitution
Lecture 5: Basics of Enolate Chemistry
Lecture 6: Reactions of Enolates with Carbonyl Electrophiles
Lecture 7: Addition to Electrophilic Alkenes; Reactions with S, P and Si, Oxidation/Reduction
Lecture 8: Heteroaromatic Chemistry, Synthesis of Functionalised Aromatic Heterocycles

The content of the lectures has been developed by academic experts in the field of synthetic organic chemistry, and the course consists of a combination of lectures, practising with exercises and a written exam.

Teacher(s)

Teachers

Prof. dr. Floris Rutjes

Professor Synthetic Organic Chemistry

Prof. dr. Floris Rutjes is a specialist in the synthesis of organic molecules. He focuses on:

Developing new and sustainable (catalytic) synthesis methodology;
The design and synthesis of biologically active small molecules;
New click-probes for bio-orthogonal conjugation.

Dr. Pedro Hermkens

Pedro Hermkens (PhD) has a scientific background in organic chemistry, pharmacology and biochemistry. He worked at Organon, Schering-Plough and MSD (Merck) in the Medicinal Chemistry Department for 21 years were he was responsible for projects in several therapeutic areas as team leader. Furthermore, he has experience in the early stage of the process as Discovery Leader. In this role he was responsible for managing target identification & validation, assay development, screening & hit identification & optimization. The last few years he was section head Lead Optimization (Director Medicinal Chemistry) managing 3-4 project teams in parallel from lead to development candidate in different therapeutic areas; immunology, oncology and women’s health. During his career he was heavily involved in combinatorial chemistry, automation of chemistry and library design.

In 2008 he was appointed as extraordinary professor Medicinal Chemistry at Radboud University Nijmegen and in 2013 became director of the Institute Applied BioSciences & Chemistry of the HAN University of Applied Sciences. In 2020 he accepted the position of lector(Applied professor) Drug Discovery at the same university . He is currently retired, but still advisor of Pivot Park.