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Fluoroalkyl Amino Reagents for the Introduction of the Fluoro(trifluoromethoxy)methyl Group onto Arenes and Heterocycles
Organic Letters ( IF 4.9 ) Pub Date : 2017-09-01 00:00:00 , DOI: 10.1021/acs.orglett.7b02444 Etienne Schmitt 1 , Sébastien Bouvet 2 , Bruce Pégot 2 , Armen Panossian 1 , Jean-Pierre Vors 3 , Sergii Pazenok 4 , Emmanuel Magnier 2 , Frédéric R. Leroux 1
Organic Letters ( IF 4.9 ) Pub Date : 2017-09-01 00:00:00 , DOI: 10.1021/acs.orglett.7b02444 Etienne Schmitt 1 , Sébastien Bouvet 2 , Bruce Pégot 2 , Armen Panossian 1 , Jean-Pierre Vors 3 , Sergii Pazenok 4 , Emmanuel Magnier 2 , Frédéric R. Leroux 1
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Fluoroalkyl amino reagents 1a and 2a have been developed from commercially available trifluoromethyl trifluorovinyl ether via a hydroamination reaction with diethylamine or dimethylamine. These reagents can be activated by treatment with a Lewis acid and subsequently used as a mono- or dielectrophile for the introduction of the fluoro(trifluoromethoxy)methyl group, either in Vilsmeier-type acylations of aromatic substrates or in the synthesis of fluorinated pyrazoles from CH-acidic substrates and of bis-fluorinated pyrazoles, all being important building blocks for medicinal and agricultural chemistry.
中文翻译：
用于将氟（三氟甲氧基）甲基引入芳烃和杂环的氟烷基氨基试剂
氟代烷基氨基试剂1a和2a是通过与二乙胺或二甲胺的加氢胺化反应从市售的三氟甲基三氟乙烯基醚开发而来的。这些试剂可通过用路易斯酸进行处理而活化，然后在芳香族底物的Vilsmeier型酰化反应中或从CH合成氟化吡唑的过程中，用作引入氟（三氟甲氧基）甲基的单亲电体或双亲电体。 -酸性底物和双氟化吡唑，都是药物和农业化学的重要组成部分。
更新日期：2017-09-01
中文翻译：
用于将氟（三氟甲氧基）甲基引入芳烃和杂环的氟烷基氨基试剂
氟代烷基氨基试剂1a和2a是通过与二乙胺或二甲胺的加氢胺化反应从市售的三氟甲基三氟乙烯基醚开发而来的。这些试剂可通过用路易斯酸进行处理而活化，然后在芳香族底物的Vilsmeier型酰化反应中或从CH合成氟化吡唑的过程中，用作引入氟（三氟甲氧基）甲基的单亲电体或双亲电体。 -酸性底物和双氟化吡唑，都是药物和农业化学的重要组成部分。
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