H. Maruoka, N. Kashige, Takafumi Eishima
Nov 1, 2008
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0
Influential Citations
20
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Journal
Journal of Heterocyclic Chemistry
Abstract
A series of new spiro[cyclopropane-1,4′-pyrazol-3-one] derivatives 3a-h were synthesized by the reaction of 4-arylidene-3H-pyrazol-3-one 1 with secondary and tertiary carbanions derived from a methylene and methine group bearing both a leaving group and electron-withdrawing group, e.g. methyl chloroacetate, ethyl chloroacetate, isopropyl chloroacetate, tert-butyl chloroacetate, chloroacetonitrile, 2-chloro-N,N-diethylacetamide, methyl 2-chloropropionate and 2-chloropropionitrile, in the presence of sodium hydride. All the synthesized compounds 3a-h were active against Candida albicans with MIC ≤ 25 μg/mL in vitro.