Abstract
AbstractThe free radical addition of thioacetic acid to 1,2‐dicarbethoxy‐1,2,3,6‐tetrahydropyridazines gave high yields of 1,2‐dicarbethoxy‐4‐S‐thiolacetoxypiperidazines. The latter compounds served as the key intermediates in the preparation of 4‐piperidazinethiols. The thiolacetoxy derivatives were partially hydrolyzed to afford the related 1,2‐dicarbethoxy‐4‐piperidazinethiols. Complete hydrolysis of the thiolacetates gave rise to 4‐piperidazinethiols. Finally, lithium aluminum hydride reduction of the thiolacetoxy esters produced a series of 1,2‐dimethyl‐4‐piperidazinethiols. Only 4‐piperidazinethiol hydrochloride showed appreciable anti‐radiation activity.
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