Synthesis of Drugs

Code:

Q4114

Acronym:

Q4114

Level:

400

Keywords
Classification	Keyword
OFICIAL	Chemistry

Instance: 2023/2024 - 2S

Active?	Yes
Web Page:	http://https://sigarra.up.pt/fcup/pt/ucurr_geral.ficha_uc_view?pv_ocorrencia_id=528339
Responsible unit:	Department of Chemistry and Biochemistry
Course/CS Responsible:	Master in Biochemistry

Cycles of Study/Courses

Acronym	No. of Students	Study Plan	Curricular Years	Credits UCN	Credits ECTS	Contact hours	Total Time
M:BQ	6	Plano de Estudos do MBIOQ_2013-2014	1	-	6	56	162

Teaching language

Portuguese

Objectives

General: Provide valuable knowledge of organic and pharmaceutical chemistry, applied in the preparation of drugs, as a vocational training component in the field of chemistry of bioactive compounds.
 
Specific: A) Structure of organic compounds and functional groups; B) Basic nomenclature in organic chemistry; C) Stereochemistry and its biological importance; D) Synthesis and reactivity of organic compounds; E) Organic compounds of biological interest and families of drugs.

Learning: A) Essential and present reactions for the organic synthesis of drugs classified by pharmacological activities; B) Strategies for the synthetic and tridimensional (stereochemistry) design of drugs; C) Notions for the study of the relation structure and biological activity of drugs (SAR) in the development of new drugs; D) In ​​laboratory classes, through the development of mini-projects, basic and current techniques of preparation of new drugs will be learned.

Learning outcomes and competences

Once this course has been planned to introduce and develop fundamental concepts of organic synthesis of the main families of drugs (organic molecules associated with its pharmacological activities).  In addition to explain these reasons, appear to design synthetic strategies and the stereochemistry associated with such strategies of organic synthesis.
It also demonstrates the application of data and concepts presented in solving chemical problems and the role that organic chemistry plays in the development of new drugs.
In laboratory classes, the basic techniques of isolation, purification and identification of organic compounds are seized by performing mini projects connected with current research taking place in our labs DQB.

Working method

Presencial

Program

Lectures:
1.  HALOGENATION REACTIONS
2. SUBSTITUTION AND ELIMINATION REACTIONS
3. AMINES
4. ALCOHOLS
5. ALKENES
6. AROMATIC SYSTEMS
7. CARBONYL GROUP
8.CARBOXYLIC DERIVATIVES
9. PROTECTING GROUPS
10. CARBAMATES
11: GUANIDINES
12. CYCLOPROPANES AND CYCLOBUTANES
13. BENZOIC ACID DERIVATIVES
14. ACETIC ACID DERIVATIVES
15. ARILSULFONAMIDES AND SULPHONYLUREAS
16. ETHYLAMINE DERIVATIVES. DIARYLPROPYLAMINAS.
17. ETHYLAMINE DERIVATIVES..
18. ETHYLAMINE DERIVATIVES.. OXIETHYLAMINAS
19. PYRIDINE and PYRIMIDINE DERIVATIVES
20. PENTACYCLIC PI-EXCESS SYSTEMS.
21. QUINOLINE DERIVATIVES
22. ISOQUINOLINE DERIVATIVES
23. QUINAZOLINES AND  QUINAZOLONES
24. BENZIMIDAZOLE DERIVATIVES

PRACTICAL SECTION (mini-projects):
- Secoesteroides
- Bioactive peptides
- Glucuronides
- Primaquine derivatives
- Neuroprotective agents
- Chiral auxiliaries
- Prolinomimetic tripeptides
- Surfactants derived from amino acids
- Nucleoside analogues
- Synthesis of coelenterazine luminescent analogues

Mandatory literature

Vollhardt, K. P. e Shore, N. E., W. H. Freeman and Company.; ORGANIC CHEMISTRY
D. C. Eaton, Mc Graw-Hill Book Company, 1989; " Laboratory Investigations in Organic Chemistry"
Clayden, Greeves, Warren and Wothers; Oxford (www.oup.com); ORGANIC CHEMISTRY

Complementary Bibliography

Schore, N. E, Ed,. W. H. Freeman and Company. ; “Organic Chemistry - Study Guide and Solutions Manual"
C. Afonso, D. Simão, L. Ferreira, M. E. Serra, M.M. Raposo, C. Afonso, D. Simão, L. Ferreira, M. E. Serra, M.M. Raposo, IST Press, 2011; "100 experiências de química orgânica"
Mc Murry, J., Brooks/Cole Publishing Company.; ORGANIC CHEMISTRY
Mc Murry, S., Ed., Brooks/Cole Publishing Company. ; “Organic Chemistry-Study Guide and Solutions Manual”

Comments from the literature

During the semester will be provided material support classes and other bibliographic sources.

Teaching methods and learning activities

Type of evaluation:  Continuous distributed
Terms of frequency:  in accordance with the Statutes.
Evaluation:
1) Realization of 3 frequencies (A, B and C) as exercises with a duration of 2 hours. These exercises can be carried out with bibliographic consultation.
Note = average of the frequency notes made by the student.
2) Performing home exercises.
Note = average of the completed exercises (E).
3) Performing an individually assigned work on the synthesis of a drug (F). This work should be presented in A3 poster format. All posters will be put together for a "book_poster" which will be advertised on
Link: https://padlet.com/ivo_dias/sintesedefarmacos


Theoretical Note (NT) = 0.3 x E + 0.4 [(A + B + C) / 3] + 0.3 x F

4) The laboratory's practical classes of the discipline consists in the realization of mini-projects in the Section of Organic Chemistry of the Department.
PRACTICAL NOTE (NP)
FINAL CLASSIFICATION (NF) = 0.75 x NT + 0.25 x NP

keywords

Physical sciences
Physical sciences > Chemistry > Applied chemistry > Pharmaceutical chemistry

Evaluation Type

Distributed evaluation without final exam

Assessment Components

designation	Weight (%)
Exame	20,00
Participação presencial	10,00
Teste	22,50
Trabalho escrito	22,50
Trabalho laboratorial	25,00
Total:	100,00

Amount of time allocated to each course unit

designation	Time (hours)
Apresentação/discussão de um trabalho científico	2,00
Elaboração de relatório/dissertação/tese	14,00
Estudo autónomo	28,00
Frequência das aulas	56,00
Trabalho de campo	4,00
Trabalho de investigação	14,00
Trabalho escrito	30,00
Trabalho laboratorial	14,00
Total:	162,00

Eligibility for exams

Regulation of FCUP

Calculation formula of final grade

FINAL STANDINGS (NF) = 0.7 5x NT + 0.25 x NP

Examinations or Special Assignments

Regulation of FCUP

Special assessment (TE, DA, ...)

Regulation of FCUP

Classification improvement

Regulation of FCUP

Observations

Type classes: Theoretical (2 h / week);
Type classes: theoretical-practical (exercices) (1 h/ week)
Type classes: Laboratory Practice (1 h / week) with flexible hours.