chapter  9
12 Pages

Structure–Activity Relationships of Peroxide-Based Artemisinin Antimalarials

ByMitchell A. Avery, Graham McLean, Geoff Edwards, Arba Ager

The biosynthesis of artemisinin3 is of interest in that it provides clues to the chemical synthesis of artemisinin from its more abundant precursor in A. annua, artemisinic acid 2. Conjugate reduction of the acrylate double bond of 2 followed by singlet oxygenation leads,

after acidification, to the production of artemisinin.4 While percentages as high as 2.6% have been quoted for isolation of artemisinic acid,5 anecdote suggests that drying of plant material must occur in the dark. Material dried in the sun contains very little 2.