Novel Ultrasound-Promoted Parallel Synthesis of Trifluoroatrolactamide
Library via a One-Pot Passerini/Hydrolysis Reaction Sequence and Their
Fungicidal Activities
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Abstract
An ultrasound-promoted one-pot Passerini/hydrolysis
reaction sequence has been developed for the synthesis of trifluoroatrolactamide
derivatives using a diverse range of trifluoroacetophenones and isonitriles
in acetic acid. Parallel synthesis in a centrifuge tube using a noncontact
ultrasonic cell crusher was used in this study as an efficient method
for the rapid generation of combinatorial trifluoroatrolactamide libraries,
and subsequent biochemical evaluation of the resulting compounds indicated
that they possessed excellent broad-spectrum fungicidal activities. <i>N</i>-(4-chlorophenyl)-2-(4-ethylphenyl)-3,3,3-trifluoro-2-hydroxypropanamide
and <i>N</i>-(4-chlorophenyl)-3,3,3-trifluoro-2-hydroxy-2-(4-methoxyphenyl)propanamide,
in particular, showed significant fungicidal activities against all
of the fungal species tested in the current study