SYNTHESIS AND BIOLOGICAL-ACTIVITY OF THIOBASIDALIN

Thiobasidalin 2, the thiolactone analogue of the antibiotic basidalin 1, is synthesized starting from easily accessible thiotetronic acid 3 via a straightforward reaction sequence employing the chemoselective l ithium aluminum hydride reduction of the acid pyrazolide 31 as the fin al key step. Antimicrobial tests reveal that thiobasidalin 2 as well a s a number of its synthetic congeners display considerable activity ag ainst both eucaryontes and procaryontes. (C) Elsevier, Paris.