Synthesis and fungicidal activity of enantiomerically pure (R)- and (S)-silicon-containing azole fungicides.

Abstract:

:Enantiomerically pure (R)- and (S)-1-(1H-1,2,4-triazol-1-yl)-2-(4-fluorophenyl)-3-trimethylsilylpropan-2-ol 1 were prepared via an enantioselective Grignard reaction. The absolute stereochemistry of 1 was determined by X-ray analysis. In a comparison of in vitro antifungal activities of the enantiomers, the (-)-enantiomer with the R-absolute configuration was far more potent than the (+)-enantiomer.

journal_name

Bioorg Med Chem

authors

Itoh H,Furukawa Y,Tsuda M,Takeshiba H

doi

10.1016/j.bmc.2004.04.027

subject

Has Abstract

pub_date

2004-07-01 00:00:00

pages

3561-7

issue

13

eissn

0968-0896

issn

1464-3391

pii

S0968089604003165

journal_volume

12

pub_type

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