An efficient preparation of novel 5-fluoropyrazolin-3-one derivatives from α-trifluoromethylated α-arylacetates

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• 作者：Park ; No Kyun ; Kim ; Bum Tae ; Moon ; Surk Sik ; Jeon ; Sung Lan ; Jeong ; In Howa
• 关键词：Fluoropyrazoles ; 2 ; 2-Difluorovinyl ketones ; α ; -Arylacetates
• 刊名：Tetrahedron
• 出版年：2004
• 期刊代码：107_00404020
• 类别：ch
• 出版时间：August 30, 2004
• 卷：60
• 期：36
• 页码：7943-7949
• 文件大小：173 K

摘要

The reactions of α-trifluoromethylated α-arylacetates 1 with 3equiv of hydrazine, methylhydrazine or benzylhydrazine in 1,4-dioxane at reflux for 24 h afforded the corresponding 5-fluoropyrazolin-3-one derivatives 3a–m in high yields. Similarly, treatment of 1 with 3equiv of PhNLiNH₂ in THF at −78 °C, followed by warming to room temperature, resulted in the formation of 3n–s in high yields.