Ciro MILITE | PRACTICE TO SYNTHETIC METHODS IN MEDICINAL CHEMISTRY
Ciro MILITE PRACTICE TO SYNTHETIC METHODS IN MEDICINAL CHEMISTRY
cod. 0760400023
PRACTICE TO SYNTHETIC METHODS IN MEDICINAL CHEMISTRY
| 0760400023 | |
| DIPARTIMENTO DI FARMACIA | |
| EQF7 | |
| PHARMACEUTICAL CHEMISTRY AND TECHNOLOGY | |
| 2024/2025 |
| OBBLIGATORIO | |
| YEAR OF COURSE 4 | |
| YEAR OF DIDACTIC SYSTEM 2023 | |
| SPRING SEMESTER |
| SSD | CFU | HOURS | ACTIVITY | |
|---|---|---|---|---|
| CHIM/08 | 3 | 24 | LESSONS | |
| CHIM/08 | 3 | 36 | LAB |
| Objectives | |
|---|---|
| THE COURSE AIMS TO PROVIDE STUDENTS WITH THEORETICAL AND PRACTICAL KNOWLEDGE OF THE MAIN SYNTHETIC APPROACHES USED IN THE PHARMACEUTICAL FIELD KNOWLEDGE AND UNDERSTANDING AT THE END OF THE COURSE THE STUDENT WILL KNOW: - THE CORRECT USE OF CHEMICAL REAGENTS IN COMPLIANCE WITH GENERAL SAFETY REGULATIONS - THE CORRECT USE OF SEARCH ENGINES TO CARRY OUT BIBLIOGRAPHIC RESEARCHES IN ALL FIELDS OF CHEMISTRY (EG SCIFINDER) - THEORETICAL AND PRACTICAL ASPECTS OF THE CLASSICAL (OR TRADITIONAL) SYNTHETIC APPROACH - THEORETICAL AND PRACTICAL ASPECTS ON THE SYNTHESIS ON SUPPORT AND SUPPORT-ASSISTED SYNTHESIS - GREEN CHEMISTRY APPROACHES -THE MAIN INNOVATIVE SYNTHETIC PROCEDURES EMPLOYED IN MEDICINAL CHEMISTRY APPLYING KNOWLEDGE AND UNDERSTANDING AT THE END OF THE COURSE THE STUDENT WILL BE ABLE TO: -PERFORM A BIBLIOGRAPHIC RESEARCH -DESIGN A SYNTHETIC SCHEME -MAKE SIMPLE CHEMICAL REACTIONS FOLLOWING PROCEDURES REPORTED IN THE LITERATURE - USE THE MAIN METHODS OF PURIFICATION AND ISOLATION OF SYNTHETIC ORGANIC COMPOUNDS MAKING JUDGMENTS: THE STUDENT WILL BE ABLE TO: -CRITICALLY EVALUATE FACTORS ENABLING FOR A SCALE-UP SYNTHESIS -PREDICT THE ENVIRONMENTAL IMPACT OF A SPECIFIC SYNTHETIC APPROACH -SUGGEST A SYNTHETIC SCHEME AND A SYNTHETIC PROCEDURE ENABLING FOR A FAST AND WIDE EXPLORATION OF THE CHEMICAL SPACE USEFUL FOR DRUG DISCOVERY AND/OR DRUG OPTIMIZATION ALSO IN INDUSTRIAL FIELD -USE THE ACQUIRED KNOWLEDGE IN MULTIDISCIPLINARY PROCESSES AT THE INTERFACE BETWEEN CHEMISTRY AND BIOLOGY COMMUNICATION SKILLS THE STUDENT WILL BE ABLE TO PRESENT A SYNTHESIS PROJECT AND A PRACTICAL PROCEDURE IN WRITTEN AND ORAL FORM, EMPLOYING AN APPROPRIATE TECHNO-SCIENTIFIC TERMINOLOGY ABILITY TO LEARN THE STUDENT WILL BE ABLE TO CORRECTLY EVALUATE PROCEDURES REPORTED IN SCIENTIFIC PUBLICATIONS AND PATENTS |
| Prerequisites | |
|---|---|
| TO BE ELIGIBLE TO TAKE THE PHARMACEUTICAL SYNTHESIS LABORATORY EXAM, THE STUDENT MUST HAVE PASSED ALL THE EXAMS FROM THE FIRST AND SECOND YEAR OF THE COURSE. |
| Contents | |
|---|---|
| THE COURSE IS DIVIDED INTO A THEORETICAL PART (24 HOURS, 3 ECTS) AND A PRACTICAL PART (36 HOURS, 3 ECTS). THE THEORETICAL PART COVERS THE FOLLOWING TOPICS: - DESIGNING A SYNTHETIC METHOD. TOOLS AND DEVELOPMENT OF BIBLIOGRAPHIC RESEARCH: DATABASES AND SOFTWARE. (4 HOURS, 0.50 ECTS) - INTRODUCTION TO SYNTHESIS TECHNIQUES: SYNTHETIC STRATEGIES, EQUIPMENT FOR CHEMICAL REACTIONS, REACTION TEMPERATURE CONTROL, REAGENT ADDITION, MAGNETIC AND MECHANICAL STIRRING, USE OF INERT GASES. SPECIAL EQUIPMENT. PREPARATION OF ANHYDROUS SOLVENTS, DRYING OF SOLID SUBSTANCES. (4 HOURS, 0.50 ECTS) - SYNTHETIC PROCEDURES FOR REACTIONS IN AN ANHYDROUS ENVIRONMENT, UNDER HIGH PRESSURE, AT LOW TEMPERATURE, WITH REFLUX HEATING. (2 HOURS, 0.25 ECTS) - REACTION MONITORING: TLC AND HPLC (2 HOURS, 0.25 ECTS) - REACTION WORKUP: FILTRATION, EXTRACTION, SOLVENT REMOVAL. (2 HOURS, 0.25 ECTS) - PURIFICATION AND ISOLATION OF A REACTION PRODUCT: ACID-BASE EXTRACTION; CONTINUOUS AND SUPERCRITICAL FLUID EXTRACTORS (E.G., CO2); CRYSTALLIZATION; SUBLIMATION; SIMPLE AND FRACTIONAL DISTILLATION, AT NORMAL AND REDUCED PRESSURE; STEAM DISTILLATION; PREPARATIVE TLC, COLUMN CHROMATOGRAPHY, HPLC. (4 HOURS, 0.50 ECTS) - ADVANCED SYNTHETIC METHODOLOGIES: GREEN CHEMISTRY, DOMINO REACTIONS AND MULTICOMPONENT REACTIONS (MCR), MICROWAVE-ASSISTED REACTIONS, FLOW CHEMISTRY, ELECTROCHEMISTRY, PHOTOCHEMISTRY. (6 HOURS, 0.75 ECTS) THE PRACTICAL PART CONSISTS OF 8 SINGLE-STATION EXERCISES LASTING 4.5 HOURS EACH. SPECIFICALLY, THE FOLLOWING TOPICS WILL BE COVERED: - TLC: PREPARATION, SOLVENT SELECTION, USE FOR SEPARATING COMPLEX MIXTURES, USE OF SPOT REAGENTS (4.5 HOURS, 0.375 ECTS) - LIQUID-LIQUID EXTRACTION (4.5 HOURS, 0.375 ECTS) - CHROMATOGRAPHIC PURIFICATION (4.5 HOURS, 0.375 ECTS) - SYNTHESIS, PURIFICATION, AND CHARACTERIZATION OF PARACETAMOL (4.5 HOURS, 0.375 ECTS) - OPTIMIZATION OF ESTER HYDROLYSIS CONDITIONS (4.5 HOURS, 0.375 ECTS) - PHOTOCHEMICAL SYNTHESIS, PURIFICATION, AND CHARACTERIZATION OF BENZOPINACOL (4.5 HOURS, 0.375 ECTS) - MICROWAVE-ASSISTED ESTERIFICATION (4.5 HOURS, 0.375 ECTS) - NUCLEOPHILIC AROMATIC SUBSTITUTION REACTIONS: SYNTHESIS, PURIFICATION, AND IDENTIFICATION OF REACTION PRODUCTS (4.5 HOURS, 0.375 ECTS) |
| Teaching Methods | |
|---|---|
| THE COURSE IS DIVIDED INTO A THEORETICAL PART AND A PRACTICAL PART. THE THEORETICAL PART CONSISTS OF 24 HOURS OF LECTURES (3 ECTS), CONDUCTED IN THE CLASSROOM WITH THE AID OF PROJECTIONS. THE PRACTICAL PART CONSISTS OF 8 SINGLE-STATION EXERCISES IN THE TEACHING LABORATORY, EACH LASTING 4.5 HOURS, COVERING TOPICS ALREADY DISCUSSED THEORETICALLY IN THE CORRESPONDING LECTURES, FOR A TOTAL OF 36 HOURS (3 ECTS). BEFORE EACH LABORATORY EXERCISE, STUDENTS WILL BE DULY INSTRUCTED AND PROVIDED WITH THE RELEVANT EXERCISE MATERIALS. ATTENDANCE AT BOTH THE LECTURES AND THE EXERCISES IS MANDATORY. TO HAVE THE PRACTICAL LABORATORY PART RECOGNIZED, STUDENTS MUST ATTEND AT LEAST 80% OF THE SCHEDULED EXERCISES. |
| Verification of learning | |
|---|---|
| THE ACHIEVEMENT OF THE COURSE OBJECTIVES IS CERTIFIED THROUGH THE PASSING OF AN ORAL EXAM LASTING APPROXIMATELY 20 MINUTES, AIMED AT VERIFYING THE KNOWLEDGE ACQUIRED BY THE STUDENTS IN BOTH THE THEORETICAL AND PRACTICAL PARTS OF THE COURSE. THE INTERVIEW IS INTENDED TO ASSESS THE LEVEL OF KNOWLEDGE AND UNDERSTANDING REACHED BY THE STUDENT, AS WELL AS TO VERIFY THEIR ABILITY TO PRESENT USING APPROPRIATE TERMINOLOGY. THE EXAM IS PASSED WITH A SCORE OF AT LEAST 18 OUT OF 30. HONORS MAY BE AWARDED TO STUDENTS WHO ACHIEVE THE MAXIMUM SCORE OF 30 OUT OF 30 AND DEMONSTRATE THE ABILITY TO INDEPENDENTLY APPLY THE KNOWLEDGE AND SKILLS THEY HAVE ACQUIRED. |
| Texts | |
|---|---|
| M. D’ISCHIA LA CHIMICA ORGANICA IN LABORATORIO, ED. PICCIN; ROYSTON M. ROBERTS, JOHN C. GILBERT, STEPHEN F. MARTIN CHIMICA ORGANICA SPERIMENTALE, ED. ZANICHELLI; MICHAEL B. SMITH, JERRY MARCH ADVANCED ORGANIC CHEMISTRY, ED. WILEY INTER SCIENCE SLIDES PRESENTED DURING LECTURES BY THE INSTRUCTOR (THEY SHOULD SERVE AS A STUDY GUIDE AND CANNOT REPLACE TEXTBOOKS) WILL BE AVAILABLE ON THE TEAMS PLATFORM. |
| More Information | |
|---|---|
| FOR FURTHER INFORMATION CONTACT: CMILITE@UNISA.IT |
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