| 摘要 |
<p>Triazole derivs. (I) [R=5-Cl-2-pyridyl, (un)substd. Ph; R1=H, Me! are prepd. and have antifungal activities. Thus, 4'-chloro-2 (1H-1,2,4- triazol-1-yl)acetophenone is monohydroated with NaH and MeI to yield the propiophene compd, which is methylated with NaH and MeI to give the 2-methylpropiophenone deriv. This compd. is treated with Me3 S+(O)I- to produce 2-(4-chlorophenyl)-2-[2-(1H1,2,4-triazol-1-yl) prop-2-yl oxalane, which is treated with 1,2,4-triazole and K2CO3 to give (I)(R=4-ClC6H4, R1=Me, III). Mice infected with A. flavus treated with 20mg (III)/kg orally 1 and 4h post infection and twice daily for next 4 days have an increase in mean survival time of 15 days.</p> |
