Synthesis of 2‐Pyridyl‐α‐toluenesulfonates as Antimalarials

A series of substituted 2‐pyridyl‐α‐toluenesulfonates was synthesized for antimalarial testing. They were prepared by treating various 2‐pyridinols with α‐toluenesulfonyl chlorides in the presence of an alkali. In tests against Plasmodium berghei in mice at 640 mg/kg, only 3,5‐dichloro‐2‐pyridyl‐α‐toluenesulfonate was considered active,i.e., doubled the mean survival time.