Synthesis of New 1,2,4‐Trioxanes and their Antimalarial Activity

The three dihydronaphtho[1,2,4]trioxines 9 – 11 have been synthesized and two of them converted to the five carbamate and ester derivatives 12 – 16 ( Schemes 1 and 2 ). The resulting new trioxanes together with two already known and ascaridole ( 7 ) were tested for antimalarial activity against the sensitive N strain of Plasmodium berghei in mice. On comparison with artemisinin ( 1 ) and dihydroartemisinin ( 2 ), modest activity was found. The four most active compounds were some 12–18 times less potent than 1 .