Drug Synthesis

Recommended Prerequisites

Acquired knowledge in 1st Cycle Courses in the areas of Basic Studies in  Pharmaceutical Sciences, Medicinal Chemistry, Biochemistry, Pharmaceutical Biomedicine, Bio-analytical Sciences, Biomedical Sciences and other courses considered adequate by the Coordination of the Master Course.  

Teaching Methods

Theoretical classes, with discussion, giving relevant examples. In the theoretical-practical classes, demonstrative exercises will be presented and discussed.

Learning Outcomes

The main aim of the course "Drug Synthesis" is to transmit students concepts and experience in methods in organic and as well as crucial aspects for the training of professionals for the pharmaceutical industry of drug synthesis such as methods of optimizing the performance of processes, cost, environment and purity requirements of end products. It is a course that you want to give students knowledge / experience in design and decision-making ability in selecting the most appropriate method to implement the synthesis of pharmacologically active intermediates (API).

Work Placement(s)

No

Syllabus

Strategies and planning in organic synthesis:

Retrosynthesis Approach

Chirality and biological activity

Asymmetric Synthesis ()

Sources of chiral drugs

Catalytic processes and their Industrial Relevance

The Chemistry of Heterocyclic Compounds in Drug Development

The Importance, Diversity and Properties of Heterocyclic Compounds

Strategies for the construction of the heterocyclic ring

Examples of synthesis of Heterocyclic Drugs: Ciprofloxacin and Linezolid; Atorvastatin Calcium; Paroxetine; Orlistat, eletriptan, etc..

Perspectives in total synthesis

Total synthesis of Drugs

Examples of total synthesis of drugs: Epotilona, Quinine, Vinblastine, Quadrigemine C, Diazonamide, Vancomicine, etc.

Head Lecturer(s)

Teresa Margarida Vasconcelos Dias de Pinho e Melo

Assessment Methods

Assessment
Exam: 100.0%

Bibliography

Michael B. Smith, Organic Synthesis, 4th Ed., 2017, Academic Press; ISBN: 978-0-12-800720-4.

Petzold, D; Giedyk, M; Chatterjee, A; Konig, B; A Retrosynthetic Approach for Photocatalysis; Eur. J. Org. Chem. 2019, 1193-1244.

Patrick, G. L. An introduction to Drug synthesis, Oxford University Press, 2014.

Organic Synthesis and Molecular Engineering, Mogens Brøndsted Nielsen, 1st Ed. Wiley, 2013.

Warren, S., Wyatt, P. Organic Synthesis – the disconnection approach, 2nd edition, Wiley, 2008.

Asymmetric Synthesis: The Essentials, Edited by M. Christmann, and S. Stefan Bräse, Wiley, 2006.

Classics in Total Synthesis II: More Targets, Strategies, Methods, Ed by K.C.Nicolau, S.A. Snyder, Wiley 2003.

Heterocyclic Chemistry, T. L. Gilchrist, Longman Scientific &Technical, Third Edition, 1997.

Strategies for Organic Drug Synthesis and Design, 2º Ed., Daniel Lednicer, wiley, 2009.