MChem Chemistry with Medicinal Chemistry

Year of entry: 2021

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Course unit details:
Synthesis for Drug Discovery and Development

Unit code CHEM30442
Credit rating 10
Unit level Level 3
Teaching period(s) Semester 2
Offered by Department of Chemistry
Available as a free choice unit? No

Overview

This course unit detail provides the framework for delivery in 21/22 and may be subject to change due to any additional Covid-19 impact.  Please see Blackboard / course unit related emails for any further updates.

Lectures and workshops from staff from the School of Chemistry, AstraZeneca and the School of Pharmacy and Pharmaceutical Sciences will discuss aspects of the drug development process.

Part 1 Array chemistry Professor David J. Procter (School of Chemistry) (8 lectures)

The course will describe multicomponent couplings for the construction of arrays of medicinally-relevant  compounds. The value of the multicomponent couplings will be illustrated through examples of their application in several case studies. In addition, high-throughput methods for the synthesis of compound collections or libraries for medicinal chemistry will be described. Topics covered will include, solid-phase organic synthesis, supported reagents, combinatorial synthesis and parallel synthesis.

 

Part 2 Process Chemistry Dr Matthew Ball (AstraZeneca, Macclesfield) (8 lectures)

This series of lectures will focus on the role of the Process Chemist in pharmaceutical development, starting with drug discovery projects and producing kilo-lab, plant and multi-ton campaigns for established products. Using the framework of the SELECT criteria (Safety, environmental, legal, economic, control and throughput), real industrial case studies will be presented, aiming to show that there are very few areas of organic chemistry which cannot be developed at scale. This course also aims to display the importance of route evaluation and selection alongside good mechanistic and process understanding in the development of robust large-scale manufacturing processes.

 

Part 3 The drug development workshop Prof Leon Aarons (Pharmacy and Pharmaceutical Sciences) (6 h workshop)

 

 

Pre/co-requisites

Unit title Unit code Requirement type Description
Fundamentals of Biochemistry BIOL10551 Pre-Requisite Compulsory
Properties of Medicines PHAR10102 Pre-Requisite Compulsory
Fundamentals of Drug Discovery CHEM20421 Pre-Requisite Compulsory
The Big Killers PHAR20302 Pre-Requisite Compulsory
Advanced Drug Discovery CHEM30441 Pre-Requisite Compulsory

Aims

The unit aims to:

1. Discuss recent advances in the synthesis of compound “arrays” for drug discovery (Part 1).

2. Study the role of the process chemist in drug development (Part 2).

3. Give an overview of drug development through an intensive workshop (Part 3).

 

Learning outcomes

On successful completion of the course students should be able to:

 

  • Understand a variety of multicomponent coupling reactions for the synthesis of compound arrays.
  • Appreciate the modern techniques used in medicinal chemistry for the synthesis of compound libraries for evaluation.
  • Be able to apply the use of solid-supports and solid-supported reagents to solve synthetic problems.
  • Have a good basic understanding of the role of the Process Chemist in converting lab scale chemistry and route concepts to the pilot plant in a safe and robust manner.
  • Build on existing synthetic and mechanistic knowledge in organic chemistry, and gain an appreciation of the use of known and new chemistry and techniques in route design and selection.
  • Understand the pharmaceutical industry in terms of mid to late stage development as well as the main areas of consideration on scaling reactions appropriately

Teaching and learning methods

Lectures plus a two-day drug discovery workshop taken within the School of Pharmacy

Transferable skills and personal qualities

Problem solving, time management, data handling and interpretation

 

Assessment methods

Method Weight
Written exam 80%
Set exercise 20%

Feedback methods

Part 1 Revision problem sheet – handed in and feedback given by the Lecturer remotely or through one-to-one meetings

Part 2 Revision Workshop – feedback from interaction with Lecturer

Part 3 Drug Development Workshop – feedback from interaction with workshop staff

 

Study hours

Scheduled activity hours
Assessment written exam 2
Lectures 16
Practical classes & workshops 8
Independent study hours
Independent study 74

Teaching staff

Staff member Role
David Procter Unit coordinator

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