Master in Medicinal and Biopharmaceutical Chemistry

Advanced Topics in Drug Synthesis

ECTS

6

Learning outcomes

Discovery of new drugs is highly dependent on the capacity to design and build complex organic molecules by efficient synthetic methodologies. This knowledge is crucial during in several stages of medicinal chemistry including hit discovery, hit-to-lead optimization, and scale-up development needed for preclinical assays.

The specific aims of this course are to gain competences on:
1) Strong background on modern synthetic methodologies applied to the synthesis of drugs;
2) Rational design and implementation of state of the art synthetic routes for the preparation of therapeutic useful molecules;
3) Drug synthesis at industry, a close contact with R&D department of Portuguese pharmaceutical industries;
4) Advanced laboratory skills by engaging the students in a research project of the Drug Design program area of iMed.ULisboa research center.

Syllabus

Retrosynthetic analysis; classical interconversion of functional groups; disconnections of C-X bonds, 1,1-, 1,2-, 1,4-, 1,5- and 1,6- difuncional molecules; C-C disconnections;
- More sustainable organic synthesis; scale-out vs scale-up approaches;
-Modern catalytic transformations promoted by metal, organometals, organocatalysts and enzymes for more relevant synthetic transformations;
- Molecular rearrangements;
- Pericyclic reactions;
- More efficient protective groups of OH, diols, NH, ketones, aldehydes, carboxylic acids, alkenes and alkynes.

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