Abstract
Abstract5‐Carbapterocarpens, one of them displaying estrogenic activity, were prepared from α‐aryltetralones in high yields through a one‐pot, BBr3‐promoted O‐demethylation and cyclization sequence. The key α‐aryltetralone intermediates were obtained by direct α‐arylation of tetralones with o‐alkoxybromoarenes in the presence of Pd2(dba)3 (2.5 mol‐%) and tBu3PHBF4 (10 mol‐%) as catalysts, together with 2.5 equiv. of KOH in dioxane/H2O (4:1), under microwave irradiation conditions (80 W, 100 °C, 40 min), leading to α‐monoaryltetralones in good yields.
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