This dissertation describes new synthetic tools for high-throughput medicinal chemistry. The design of selenium-, tellurium-, and bismuth-based solid-phase linkers makes it possible to synthesize small organic molecules with pre-defined molecular architectures and functionalities. Iron-assisted nucleophilic aromatic substitution reactions on solid phase play a decisive role in the synthesis of heteroatom-substituted N-phenylpiperazines and in the serendipitous discovery of the antidepressant Brintellix® (INN: vortioxetine; code number Lu AA21004). Another highlight is the formulation of solid and liquid chemicals in the form of tablets (ChemDose™), which enables safe, accurate, and reproducible distributions of building blocks, reagents and catalysts in parallel organic synthesis.
|Advisor:||Bjarklev, Anders O.|
|School:||Polytekniske Laereanstalt, Danmarks Tekniske Hojskole (Denmark)|
|Source:||DAI-B 75/06(E), Dissertation Abstracts International|
|Subjects:||Organic chemistry, Chemical engineering, Medicine, Pharmacy sciences|
|Keywords:||Brintellix, ChemDose, LuAA21004, LuAA24530, Organic synthesis, Tedatioxetine, Vortioxetine|
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