Bridged 1,2,4-Trioxolanes: SnCl<sub>4</sub>—Catalyzed Synthesis and an In Vitro Study against <i>S. mansoni</i>

oleh: Peter S. Radulov, Ivan A. Yaremenko, Jennifer Keiser, Alexander O. Terent’ev

Format: Article
Diterbitkan: MDPI AG 2023-06-01

Deskripsi

A synthesis of bridged 1,2,4-trioxolanes (bridged ozonides) from 1,5-diketones and hydrogen peroxide catalyzed by SnCl<sub>4</sub> was developed. It was shown that the ratio of target ozonides can be affected by the application of SnCl<sub>4</sub> as a catalyst and varying the solvent. A wide range of bridged 1,2,4-trioxolanes (ozonides) was obtained in yields from 50 to 84%. The ozonide cycle was moderately resistant to the reduction of the ester group near the peroxide cycle to alcohol with LiAlH<sub>4</sub>. The bridged ozonides were evaluated for their antischistosomal activity<b>.</b> These ozonides exhibited a very high activity against newly transformed schistosomula and adult <i>Schistosoma mansoni</i>.