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Dissertation/Thesis Abstract

New Tools for High-Throughput Organic Synthesis
by Ruhland, Thomas, Dr.Techn., Polytekniske Laereanstalt, Danmarks Tekniske Hojskole (Denmark), 2013, 185; 3585065
Abstract (Summary)

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.

Indexing (document details)
Advisor: Bjarklev, Anders O.
School: Polytekniske Laereanstalt, Danmarks Tekniske Hojskole (Denmark)
School Location: 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
Publication Number: 3585065
ISBN: 978-1-303-77090-6
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