Chimie organique pharmaceutique

I. INTRODUCTION

I.A. Organic chemistry and pharmacy

I.B. The carbon atom

I.C. Interactions in organic chemistry

II. ISOMERY AND STEREOISOMERY

III. MAIN FUNCTIONAL GROUPS AND MOIETIES IN ORGANIC CHEMISTRY

IV : ANALYTICAL ASPECTS OF ORGANIC CHEMISTRY

IV.A. : Spectroscopic analysis : fluorescence

IV.B. : solid state analysis

V. ORGANIC SYNTHESIS APPLIED TO PHARMACEUTICAL SCIENCE

V.A. Main reactions in pharmaceutical sciences : nucleophilic substitution, oxidation, reduction, coupling reaction catalyzed by metals

V.B. Main chemical processes used in drug synthesis : hemisynthesis, asymmetric synthesis and separation techniques.

V.C. Impurities in the synthesis of drugs.

The course aims at giving to the students the knowledge of organic chemistry which will allow them not only to understand the subject of the courses of the present and next years but also to have a general vision of the importance of organic chemistry in the pharmaceutical world. The course is essentially based on the study and the understanding of the chemical phenomena which contribute in the manufacturing, the stability, the identification, the analysis and the mechanism of action of drugs.

Required and corequired courses

Courses requiring this course

Theory : 3 ECTS - Exercise : 1 ECTS.

The course is given ex-cathaedra with, whenever it is possible, the use of simple and non-hazardous demonstrations and chemical experiments illustrating directly certain notions seen during the course.

Exercises allow a first contact with the European Pharmacopoeia. They are based on studies of organic drugs monographs, only from the point of view of the chemistry of the molecule and not instrumental analysis.

The tackled questions contain:

- understanding of the chemical naming,

- description of possible stereoisomers,

- description of the functions and the relation with the stability of the molecule,

- possible chemical reactions of identification,

- function assayed and mechanism used for the dosage,

- synthesis of the product (when the methods of synthesis are seen in the course),

- origin of the degradation products,

- diverse questions about the subjects seen in the course (structure and properties of solvents, polarity of solvents, origin of the physico-chemical phenomena, ...)

Warning! No corrected exercise is given outside exercise sessions! Issues related to the resolution of exercises should be asked by direct contact with the owner (mail, telephone or appointment) or via the forum questions available on the Univeristé Virtuelle!

Contribution to the teaching profile

• Use a set of concepts and knowledges in health and pharmaceutical sciences. Use knowledges in anatomy, biology, chemistry, mathematics, physics, biochemistry, molecular biology, botany, analytical chemistry, pharmaceutical chemistry physiology ... for problem solving.

• Solve problems using pharmaceutical knowledge and critical thinking. Perform analysis on pharmaceutical raw materials or excipients X or any active ingredient X.

• Communicate appropriately, efficiently, accurately and with respect in a professional perspective. Adapt his language to his interlocutor (colleague, subcontractor, applicant ...)

References, bibliography, and recommended reading

● « March's Advanced Organic Chemistry: Reactions, Mechanisms, and Structure », 6th Edition, Michael B. Smith, Jerry March, Wiley.

● « Chimie Organique », Jonathan Clayden, Nick Geeves, Stuart Warren, ISBN: 0-198-50346-6, Oxford University Press

● « Organic Mechanisms - Reactions, Stereochemistry and Synthesis », Reinhard Brückner,

ISBN: 978-3-642-03650-7, Springer.

● « Traité de chimie organique », 5e édition 2009, Neil E. Schore, K. Peter C. Vollhardt, De Boeck.

● « Identification spectrométrique de composés organiques », 2e édition 2007, David J. Kiemle, Robert M. Silverstein, Francis X. Webster, De Boeck.

● « Chimie organique avancée : Structures moléculaires et mécanismes réactionnels » 1re édition 1996, Francis A. Carey, Richard J. Sundberg, De Boeck.

● « Stéréochimie et chiralité en chimie organique », 1re édition 1999, Claude Rabiller, Gérard Martin, Maryvonne Martin, De Boeck

Contacts

FRANCOIS DUFRASNE (dufrasne@ulb.ac.be)

Unité de Microbiologie, Chimie Bioorganique et Macromoléculaire.

Département de Recherche et de Développement de Médicaments

Faculté de Pharmacie - Université Libre de Bruxelles

Campus plaine - CP 205/5 - 1050 - Brussels - Belgium

Tel. 003226505235 - Fax 003226505249 - Mobile 0032473766148

Method(s) of evaluation

• Other

Other

Written examinations (January and August): approximatively 10 theoretical questions and 10 questions in the form of exercises such as those presented during the year (monograph).

Mark calculation method (including weighting of intermediary marks)

A single mark on 20 from the written exam.

Each question is scored on 0.5, 1 or 2 depending on the expected level of response. The intermediate mark is calculated from the total marks for the entire examination and then recalculated to 20 for the final mark.

Warning: depending on the quality of incorrect response given (eg, errors considered serious in terms of the importance of the covered concepts or their fundamental aspect regarding the level of study) or the quality of expression answers (eg, globaly for the examination: poorly organized answers, not correctly written, or nebulous meaning), additional points may be withdrawn without exceeding 2/20 on the final mark.

Language(s) of evaluation

• french