Synthesis of New Antimalarial 2-Pyridyl Arylalkanesulfonates.
Final rept. 1 Jul 73-30 Jun 74,
INTERNATIONAL MINERALS AND CHEMICAL CORP LIBERTYVILLE ILL
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A series of 30 2-pyridyl alpha-toluenesulfonates were prepared for antimalarial testing. These compounds are structural variations of an IMC material, 3,5-dichloro-2-pyridyl alpha-toluenesulfonate Ay 46069, which had been submitted earlier and found to have activity against P. berghei in mice. Modifications of Ay 46069 made consisted of introducing one or more groups in the alpha-toluenesulfonyl moiety Br, Cl, F, CF3, CH3 as well as replacement of the Cl in the pyridine ring by Br, CH3O, CH3, and NO2. In some instances a third substituent Cl, CH3 was placed in the 4- or 6-position of the pyridyl group. In one case, N-sulfonation occurred.
- Organic Chemistry