Abstract

An efficient [3+2] cycloaddition reaction of trifluoromethylated N-acylhydrazones with dimethyl maleate has been developed under basic conditions. This protocol provides an easy access to potentially bioactive trifluoromethylated pyrazolidines in moderate to excellent yields. It also illustrates that the trifluoromethylated N-acylhydrazones are useful trifluoromethyl building blocks for the synthesis of trifluoromethylated N-heterocycles.

An efficient [3+2] cycloaddition reaction of trifluoromethylated N-acylhydrazones with dimethyl maleate has been developed under basic conditions. This protocol provides an easy access to potentially bioactive trifluoromethylated pyrazolidines in moderate to excellent yields. It also illustrates that the trifluoromethylated N-acylhydrazones are useful trifluoromethyl building blocks for the synthesis of trifluoromethylated N-heterocycles.

中文翻译：

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[3 + 2]三氟甲基化的N-酰基hydr与马来酸酯的环加成反应：三氟甲基化的吡唑烷类化合物的合成

摘要

在碱性条件下，已经开发出三氟甲基化的N-酰基hydr与马来酸二甲酯的有效的[3 + 2]环加成反应。该方案可轻松获得潜在的具有生物活性的三氟甲基化吡唑烷，且产率中等至优异。还说明了三氟甲基化的N-酰基hydr是合成三氟甲基化的N-杂环的有用的三氟甲基结构单元。

在碱性条件下，已经开发出三氟甲基化的N-酰基hydr与马来酸二甲酯的有效的[3 + 2]环加成反应。该方案可轻松获得潜在的具有生物活性的三氟甲基化吡唑烷，且产率中等至优异。还说明了三氟甲基化的N-酰基hydr是合成三氟甲基化的N-杂环的有用的三氟甲基结构单元。