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Dichloro{4-(4-chlorophenoxy)phthalazin-1-yl} methylphosphonic dichloride
oleh: Dyhia Amrane, Omar Khoumeri, Patrice Vanelle, Nicolas Primas
Format: | Article |
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Diterbitkan: | MDPI AG 2022-09-01 |
Deskripsi
As part of our ongoing scaffold-hopping work on an antiplasmodial 2-trichloromethylquinazoline scaffold, we aimed to explore the 1-trichloromethylphthalazine scaffold as a potential new antimalarial series. Using previously chlorination conditions described by our lab to obtain a trichloromethyl group from a methyl group, we did not obtain the target compound; instead, we obtained a dichloro methylphosphonic dichloride side product <b>3</b>. The nature of this compound was then characterized by NMR, HRMS and X-ray crystallography. The same issue was previously reported by Kato et al., starting from the 2-methyl-3-nitropyridine. Finally, compound <b>3,</b> although not cytotoxic, was not active against <i>P. falciparum</i>, the parasite responsible for human malaria.