Abstract
A novel method was developed for the construction of highly functionalized indole derivatives (3), including fluorinated indoles, via a site-selective, one-pot, two-step nucleophilic aromatic substitution reaction of o-difluorobenzene derivatives (1) with heterocyclic ketene aminals (HKAs) (2) promoted by two different bases (K2CO3 and Cs2CO3). A diverse library of indoles 3 was generated in good to excellent yields using a conventional base-mediated approach rather than metal catalysts. As a result, the highly functionalized indoles were easily obtained in an environmentally friendly, rapid, and practical manner, and the products have potential biological activity.
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