Synthesis for Drug Discovery and Development


Unit code: CHEM30442
Credit Rating: 10
Unit level: Level 3
Teaching period(s): Semester 2
Offered by School of Chemistry
Available as a free choice unit?: N

Requisites

Prerequisite

Aims

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

Overview

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) (2 x 4 h workshop)

 

 

Teaching and learning methods

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

Learning outcomes

 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

Transferable skills and personal qualities

 Problem solving, time management, data handling and interpretation.

Assessment methods

  • Written exam - 80%
  • Set exercise - 20%

Feedback methods

Revision lectures and problem sheets/sessions will be held during parts 1 and 2 of the course. Feedback will be provided as part of the workshops during Part 3 of the unit.

Study hours

  • Assessment written exam - 2 hours
  • Lectures - 16 hours
  • Practical classes & workshops - 8 hours
  • Independent study hours - 74 hours

Teaching staff

David Procter - Unit coordinator

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