TEMPO催化醇经由六氟异丙酯合成相应酰胺

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醇在二氯甲烷中,TEMPO(5 mol%)催化下,被三氯异氰尿酸(1.2 eq)氧化,再在吡啶中与六氟异丙醇(2 eq)反应生成相应六氟异丙酯,14例收率53%~93%。六氟异丙酯在乙腈中与伯胺或仲胺室温下反应生成相应酰胺,20例收率81%~98%,亲核性差的伯胺或仲胺不反应。六氟异丙酯也可不分离,一锅法合成酰胺。 The alcohol is oxidized with trichloroisocyanuric acid (1.2 eq) in methylene chloride under TEMPO (5 mol%) and then reacted with hexafluoroisopropanol (2 eq) in pyridine to give the corresponding hexafluoroisopropyl ester , 14 cases yield 53% ~ 93%. Hexafluoroisopropyl ester reacted with primary or secondary amines in acetonitrile at room temperature to give the corresponding amides. The yields of 20 were 81% ~ 98%. The poorly nucleophilic primary or secondary amines did not react. Hexafluoroisopropyl ester can also be separated, one-pot synthetic amide.
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