1985 年 105 巻 6 号 p. 554-561
Ketalization of a few acetophenones with glycerol was performed with azeotropic removal of water. These ketals were benzoylated and cis compounds (1) were isolated by crystallization from methanol and condensed with imidazole, pyrazole and triazole. They were hydrolyzed to alcohols (3) and converted to the methanesulfonates (4). Imidazole derivatives (5) similar to ketoconazole were obtained from 4 by condensation of phenols and thiophenols. Antimicrobial test of the synthesized compounds (5d, fα), jα)) showed strong antimicrobial activities against Penicillium chrysogenum and Trichophyton rubrum. Most compounds synthesized had strong preventive effects against downy mildew and sheath blight. Triazole derivatives (5m, n) showed similar effects against not only such diseases but gray mould rot.