Palladium-Catalyzed Carbonylation – Catalytic Cycle

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Table of contents

1. INTRODUCTION
Drug Development
Need of Isotopic Labeling in Drug Development
Stable Isotopes in Drug Development
SIL Compounds as Clinical Agents 23 Radionuclides in Drug Development
Radioligands for Lead Discovery
Administration, Distribution, Metabolism and Excretion
Clinical Trials
Considerations in Radiochemistry 31 Carbon-14
C-14 Building Blocks
[14C]Cyanide
[14C]Acetylene
[14C]Cyanamide
[14C]Carbon Dioxide
Last-stage carboxylations developed within ISOTOPICS 41 Carbonylation in Carbon Isotope Chemistry
Palladium-Catalyzed Carbonylation – Catalytic Cycle 43 General methods for Carbonylation using [14C]Carbon Monoxide
[14C]Calcium Carbonate Pyrolysis
[14C]Formate based [14C]carbonylation chemistry
14COgen 50 Objectives
2. METHOD DEVELOPMENT: VISIBLE-LIGHT ENABLED AMINOCARBONYLATION OF UNACTIVATED ALKYL IODIDES WITH STOICHIOMETRIC CARBON MONOXIDE FOR APPLICATION ON LATE-STAGE CARBON ISOTOPE LABELING
Synthetic approaches towards carbonylation of unactivated alkyls 
Radical Carbonylation – Thermal Initiator
Nickel-Catalyzed Carbonylation
Visible-light enabled carbonylation
Aim
Development of Visible-light Enabled Palladium Catalysis
Optimization of the reaction
Investigation of the Reaction scope
Conclusion and future perspectives
3. METHOD DEVELOPMENT: REDUCTION OF 14CO2 TO 14CO, COMPARISON OF TWO METHODS 
Aim
Preliminary Results
Electroreduction of 13CO2
Reduction of 13CO2 by disilanes catalyzed by F-
Summary and Future Perspectives
4. METHOD DEVELOPMENT: RADIOSYNTHESIS OF [18F]CRIZOTINIB, A POTENTIAL RADIOTRACER FOR PET IMAGING OF THE P-GLYCOPROTEIN TRANSPORT FUNCTION AT THE BLOOD-BRAIN BARRIER 
P-glycoprotein
Positron Emission Tomography
Labeling with short-lived radionuclides
PET tracers for P-gp
Aim
Fluorine-18
Synthetic approaches
Synthesis of Precursors
Hypervalent Iodine(III) precursor
Deoxyfluorination precursor 50
Radiofluorination
Conclusion and Future Perspectives
5. SUMMARY OF FINDINGS AND FUTURE PERSPECTIVES 
6. RESUME DE LA THESE 
7. EXPERIMENTAL: VISIBLE-LIGHT ENABLED AMINOCARBONYLATION OF UNACTIVATED ALKYL IODIDES WITH STOICHIOMETRIC CARBON MONOXIDE FOR APPLICATION ON LATE-STAGE CARBON ISOTOPE LABELING 
General Information
General Reactions
Reaction Setup
Reaction mixture
Purification
Analysis
LED report of the blue LEDs
General Procedures
General Procedure for Chamber B, CO Producing Chamber
General Procedure for Aminocarbonylation Chamber A, CO Consuming Chamber
Characterization data
8. EXPERIMENTAL: REDUCTION OF 14CO2 TO 14CO, COMPARISON OF TWO METHODS General Information 
Procedures and characterization
Electrochemical reduction
Reduction of 13CO2 by disilanes catalyzed by F-
9. EXPERIMENTAL: RADIOSYNTHESIS OF 18F-CRIZOTINIB, A POTENTIAL RADIOTRACER FOR PET IMAGING OF THE P-GLYCOPROTEIN TRANSPORT FUNCTION AT THE BLOOD-BRAIN BARRIER 
General Reactions
Reaction Setup
Reaction mixture
Purification
Analysis
Radio synthesis
Quality control
Procedures and characterization data
Precursor synthesis: hypervalent iodine(III) precursor 38
Precursor synthesis: Deoxyfluorination precursor 50
Failed strategies for protection and deprotection
10. REFERENCES