Heterocyclic Medicinal Chemistry

Description: 
1. Ioannis Nicolaou: Chemical properties and synthesis of heterocyclic aromatic rings with a single heteroatom such as pyridine, quinoline, isoquinoline, pyrrole, indole and furan. Synthesis of various heterocyclic derivatives containing the above heterocyclic rings via amidation, esterification, alkylation, acylation or coupling reactions such as Sonogashira, Ulman, Suzuki, and Negishi. 2. Athina Geronikaki: Aromaticity of heterocyclic compounds. Nomenclature. Identity. Reactivity Reaction of 1,3-azoles with electrophilic reagents. 1,3-Bipolar cycloaddition. Pyrazole and its derivatives (synthetic methods, physical and spectroscopic properties, chemical properties). Imidazole (synthetic methods, physical and spectroscopic properties, chemical properties). Imidazole bioactive derivatives: histamine (synthesis, antihistamines), histidine (structure and composition, uses, analogues: 2-mercaptostidine, carnosine, pilocarpine alkaloids). Triazoles, symmetrical and adjacent (modes of synthesis, physical and spectroscopic properties, chemical properties). Its derivatives. Tetrazoles (modes of synthesis, properties, derivatives). Pentazoles. Oxazoles - Solubles (synthetic methods, physical and spectroscopic properties, chemical properties). Oxazole and thiazole derivatives. Biologically active derivatives of thiazole. Isoxazoles-Isothiazoles (synthetic methods, physical and spectroscopic properties, chemical properties). Oxadiazole (synthetic methods, properties). Mesoionic compounds (synthesis, physical and spectroscopic properties, chemical properties). Rings with various heteroatoms (1,3-dioxalanes, 1,3-dithiolanes, selenadiazoles). Generally for polyazines. Pyrimidines (synthetic methods, physical and spectroscopic properties, chemical properties). Aminopyrimidines (synthesis modes, physical and spectroscopic properties, chemical properties). Hydroxypyrimidines (synthetic methods, physical and spectroscopic properties, chemical properties) Purines (synthetic methods, physical and spectroscopic properties, chemical properties). Derivatives of pharmaceutical interest. Pyridazines (synthetic methods, physical and spectroscopic properties, chemical properties, derivatives). Pyrazine (synthetic methods, physical and spectroscopic properties, chemical properties, derivatives). Triazines (synthetic methods, physical and spectroscopic properties, chemical properties). Tetrazines. Heterocyclic analogues of benzene. Calicarenes. 3. Eleni Pontiki: Organic Microwave Assisted Organic Synthesis (MAOS) applications in organic and pharmaceutical chemistry. Basic principles of microwave irradiation as an alternative method of synthesizing new pharmaceutical compounds both in the laboratory and in the industry for green chemistry. Techniques, equipment, solvent selection, choice of basic parameters (power / time, pressure, temperature), applications and advantages and microwave phenomena. Selected microwave-based heterocyclic molecule compositions
ECTS: 
10.00
Teaching Hours: 
6
Semester: 
1