Synthesis for Drug Discovery and Development

CHEM30442 Synthesis for Drug Discovery and Development 10 Semester 2 Undergraduate Level 3 David Procter Unit coordinator Department of Chemistry 1 FHEQ level (Framework for Higher Education Qualifications) ' Last part of a Bachelors ' European Credit Transfer & Accumulation System Rating : 5.0 <div>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)</div>   <div> 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)</div>   <div> 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).</div>  On successful completion of the course students should be able to:  <ul> <li> Understand a variety of multicomponent coupling reactions for the synthesis of compound arrays.</li> <li> Appreciate the modern techniques used in medicinal chemistry for the synthesis of compound libraries for evaluation.</li> <li> Be able to apply the use of solid-supports and solid-supported reagents to solve synthetic problems.</li> <li> 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.</li> <li> 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.</li> <li> Understand the pharmaceutical industry in terms of mid to late stage development as well as the main areas of consideration on scaling reactions appropriately</li></ul> <div> Problem solving, time management, data handling and interpretation</div>  Lectures plus a two-day drug discovery workshop taken within the School of Pharmacy 1 Written exam 80% 9 Set exercise 20% <div> Part 1 Revision problem sheet – handed in and feedback given by the Lecturer remotely or through one-to-one meetingsPart 2 Revision Workshop – feedback from interaction with LecturerPart 3 Drug Development Workshop – feedback from interaction with workshop staff</div>  BIOL10551 Fundamentals of Biochemistry Pre-Requisite Compulsory PHAR10102 Properties of Medicines Pre-Requisite Compulsory CHEM20421 Fundamentals of Drug Discovery Pre-Requisite Compulsory PHAR20302 The Big Killers Pre-Requisite Compulsory CHEM30441 Advanced Drug Discovery Pre-Requisite Compulsory N Assessment written exam 2 Lectures 16 Practical classes & workshops 8 0 74