Synthesis of Unprotected β‐Arylethylamines by Iron(II)‐Catalyzed 1,2‐Aminoarylation of Alkenes in Hexafluoroisopropanol
作者:Valentyn Pozhydaiev、Marie Vayer、Claire Fave、Joseph Moran、David Lebœuf
DOI:10.1002/anie.202215257
日期:2023.2.20
Unprotected β-arylethylamines were directly accessed via 1,2-aminoarylation of alkenes under operationally simple conditions, thanks to a cooperative effect between an iron (II) catalyst and the solvent hexafluoroisopropanol. This one-pot sequential protocol did not require pre-activated (hetero)arenes and proved compatible with a broad range of drug-oriented functional groups.
由于铁 (II) 催化剂和溶剂六氟异丙醇之间的协同作用,在操作简单的条件下,通过烯烃的 1,2-氨基芳基化直接获得未保护的 β-芳基乙胺。这种一锅顺序方案不需要预激活的(杂)芳烃,并证明与广泛的药物导向功能组相容。