Beilstein J. Org. Chem.2018,14, 998–1003, doi:10.3762/bjoc.14.85
with benzophenone imine and subsequent hydrogenolysis.
Keywords: aminoestrones; Buchwald–Hartwig amination; 13α-estrone; functionalization; microwave assisted reactions; Introduction
Aminoestrones are of particular interest thanks to their diverse biological applications [1][2][3][4]. There exist
several aminated steroids in the literature, but the efficient generation of a C(sp2)–N bond on the aromatic ring A of estrone derivatives still remains a challenge. Aminoestrones substituted at C-2 or C-4 are mainly produced by the reduction or hydrogenation of the corresponding nitro derivatives [5
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Graphical Abstract
Scheme 1:
Pd-catalyzed aminations at C-2 or C-4 in the 13α-estrone series. Reactions were performed on a 0.25...