Abstract

3-Hydroxy-4-(trifluoromethyl)azetidin-2-ones were synthesized from the corresponding 3-benzyloxy-β-lactams and successfully transformed into new 3-chloro-4-(trifluoromethyl)azetidin-2-one building blocks. The latter chlorides were shown to be eligible precursors for the construction of CF₃-containing aminopropanes, 1,3-oxazinanes, 1,3-oxazinan-2-ones, and aziridines. In addition, 3-hydroxy-4-(trifluoromethyl)azetidin-2-ones proved to be interesting substrates for the synthesis of novel 3-[2,2,2-trifluoro-1-(arylamino)ethyl]-1,4-dioxan-2-ones via intramolecular cyclization of 3-(2-hydroxyethoxy)-β-lactam intermediates.

3-Hydroxy-4-(trifluoromethyl)azetidin-2-ones were synthesized from the corresponding 3-benzyloxy-β-lactams and successfully transformed into new 3-chloro-4-(trifluoromethyl)azetidin-2-one building blocks. The latter chlorides were shown to be eligible precursors for the construction of CF₃-containing aminopropanes, 1,3-oxazinanes, 1,3-oxazinan-2-ones, and aziridines. In addition, 3-hydroxy-4-(trifluoromethyl)azetidin-2-ones proved to be interesting substrates for the synthesis of novel 3-[2,2,2-trifluoro-1-(arylamino)ethyl]-1,4-dioxan-2-ones via intramolecular cyclization of 3-(2-hydroxyethoxy)-β-lactam intermediates.

中文翻译：

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3-羟基-4-（三氟甲基）氮杂环丁烷-2-酮作为制备含三氟甲基的氨基丙烷，1,3-氧杂嗪酮-2-酮，氮丙啶和1,4-二恶烷-2-酮的基础材料的用途

摘要

从相应的3-苄氧基-β-内酰胺合成3-羟基-4-（三氟甲基）氮杂环丁烷-2-酮，并将其成功转化为新的3-氯-4-（三氟甲基）氮杂环丁烷-2-酮结构单元。已显示后者的氯化物是用于构建含CF ₃的氨基丙烷，1,3-恶嗪酮，1,3-恶二嗪-2-酮和氮丙啶的合格前体。此外，3-羟基-4-（三氟甲基）氮杂环丁烷-2-酮被证明是合成新型3- [2,2,2-三氟-1-（芳氨基）乙基] -1,4-的有趣底物。二恶烷-2-酮通过3-（2-羟基乙氧基）-β-内酰胺中间体的分子内环化作用。

从相应的3-苄氧基-β-内酰胺合成3-羟基-4-（三氟甲基）氮杂环丁烷-2-酮，并将其成功转化为新的3-氯-4-（三氟甲基）氮杂环丁烷-2-酮结构单元。已显示后者的氯化物是用于构建含CF ₃的氨基丙烷，1,3-恶嗪酮，1,3-恶二嗪-2-酮和氮丙啶的合格前体。此外，3-羟基-4-（三氟甲基）氮杂环丁烷-2-酮被证明是合成新型3- [2,2,2-三氟-1-（芳氨基）乙基] -1,4-的有趣底物。二恶烷-2-酮通过3-（2-羟基乙氧基）-β-内酰胺中间体的分子内环化作用。