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  • About
  • The Global ETD Search service is a free service for researchers to find electronic theses and dissertations. This service is provided by the Networked Digital Library of Theses and Dissertations.
    Our metadata is collected from universities around the world. If you manage a university/consortium/country archive and want to be added, details can be found on the NDLTD website.
1

Attempted routes towards the synthesis of fluorinated analogues of ornithine as potential inhibitors of ornithine decarboxylase

De Villiers, Jandre 03 1900 (has links)
Thesis (MSc (Chemistry and Polymer Science))--University of Stellenbosch, 2007. / Human African Trypanosomiasis (HAT) is a disease that threatens more then 60 million men, woman and children in Africa. It is known that the inhibition of the enzyme, ornithine decarboxylase (ODC) leads to cell arrest and subsequent death of Trypanosoma brucei, the parasite that causes the disease. The fluorinated ornithine analogue, DFMO (difluoromethylornithine or eflornithine) is a known inhibitor of ODC. Although various syntheses for DFMO exist they have some practical drawbacks which prevent the cost effective production of this compound as a drug for HAT treatment. This work focuses on the synthetic preparation of the fluorinated ornithine analogue DFMO as well as the fluorinated ornithine analogues 2-MFMO, 3-fluoro-ornithine and 3,3-difluoro-ornithine. Our chosen synthetic methodology focused on the introduction of the fluorine functionality using a simpler, safer and more convenient method than current direct fluorination techniques, or those that rely on the use of CFCs. Instead we decided to develop and optimise a fluorodehydroxylation method based on the transformation of hydroxylated ornithine analogues. The fluorodehydroxylation method substitutes a hydroxyl group to the corresponding fluorine and can also be used to transform an aldehyde or ketone to the corresponding difluoro group. Application of this fluorination method requires the synthesis of appropriate ...

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