Artemisinin first generation

Artemisinin is a potent antimalarial drug belonging to the chemical class of sesquiterpenoid endoperoxide lactones. Its poor solubUity in water and organic phases has led to a focus on the development of derivatives towards increased solubility, metabohc and chemical stabUity and bioavailabihty [92]. A common feature of the first generation of artemisinin derivatives was the replacement of the ketone with bigger polar groups to form... 

In this chapter, we first describe the peculiar electronic structure of 2 and its impact on its chemical reactivity that is opposite from that of ordinary oxygen 02-Then, we compare the respective advantages and limitations of photochemical and chemical methods to generate 2 in a context of industrial development. In particular, we detail the criteria for choosing a reaction medium compatible with both the organic substrate and water-soluble chemical sources of 02- Finally, the main reactions of 2 in organic chemistry are listed and illustrated with two industrially relevant examples recently developed in the fields of perfumery (synthesis of rose oxide) and pharmacy (synthesis of artemisinin). 

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