Abstract
The present review summarizes publications on the artemisinin peroxide fragment synthesis from 1983 to 2016. The data are classified according to the structures of a precursor used in the key peroxidation step of artemisinin peroxide cycle synthesis. The first part of the review comprises the construction of artemisinin peroxide fragment in total syntheses, in which peroxide artemisinin ring resulted from reactions of unsaturated keto derivatives with singlet oxygen or ozone. In the second part, the methods of artemisinin synthesis based on transformations of dihydroartemisinic acid are highlighted.
Highlights
In accordance with World Health Organization reports, malaria is one of the most widespread diseases, with 149–303 million of new malaria cases and 438,000 malaria deaths registered in 2015 all over the world
The reaction of vinyl with ozone followed by the rearrangement of unstable peroxide intermediate provided artemisinin silane(1)51with
Ene reaction of dihydroartemisinic acid (4) 2017, with22,singlet oxygen afforded intermediate 5, which was rearranged into artemisinin 14 (1)ofby
Summary
In accordance with World Health Organization reports, malaria is one of the most widespread diseases, with 149–303 million of new malaria cases and 438,000 malaria deaths registered in 2015 all over the world. Semi-synthetic methods for artemisinin (1) production from artemisinic (3). The construction of peroxide fragment of artemisinin is carried approaches to final artemisinin production. The present review is devoted to the strategies of the artemisinin peroxide fragment in synthetic and semi-synthetic approaches Synthetic methods where dihydroartemisinic peroxidation/cyclization step in artemisinin. In 2013, the Sanofi company launched semi-synthetic artemisinin manufacturing based on photooxidation of dihydroartemisinic acid (4)the [41]. Peroxidation steps based on the formation of hydroperoxides in synthetic approaches to Scheme 1. Peroxidation steps based on the formation of hydroperoxides in synthetic approaches to artemisinin (1). In the 2present review, the data are primarily classified according to the structures of final precursors 2 and 4 and secondly according to the peroxidation methods
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