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Synthesis and antifungal activity of spiro[cyclopropane‐1,4′‐pyrazol‐3‐one] derivatives

ISSN:0022-152X
2008年第45卷第6期
Article

chemical structure image 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.

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ISSN:0022-152X
2008年第45卷第6期
Article

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