The work of this book provides us to understand that trioxanes can be a better alternative medication for Malaria. Malaria is a major parasitic disease of the tropics, affecting around 300–500 million people of which more than one million die each year. Peroxide group, present in the form of 1, 2, 4-trioxane, is essential for the anti-malarial activity. A series of 1,2,4 trioxane derivative synthesized by treating p-chloroacetophenone with ethyl 2-bromoacetate to give ethyl 3-(4-chloro phenyl)-3-hydroxy butanoate which on dehydration, yield (Z)-ethyl 3-(4-chloro phenyl) but-2 enoate. On reduction yield (Z)-ethyl 3-(4-chloro phenyl) prop-1-en-1-ol. Further on photo oxygenation it yield 3-(4-chlorophenyl)-2 hydroperoxybut-3-en-1-ol, which on condensation with ketones to give the final product. The structures of synthesized compound were confirmed on the basis of their spectral data and elemental analysis. Compounds were evaluated for antimalarial activity against Plasmodium yoelii and compared with standard drug. The final product derivatives are potent in antimalarial activity.