Aqueous amination demonstrates broad substrate scope in micellar systems, highlighting practical applications in pharmaceuticals.
An efficient micellar palladium-catalyzed aqueous Buchwald-Hartwig amination has been developed, enabled by the self-assembly of amphiphilic copolymer polyethylene glycol-polyvinylethylene glycol (PEG-PVEG). Using 0.5 mol % BrettPhos-Pd-G3 as a catalyst, the aqueous amination showed broad a substrate scope, including aryl bromides, aryl chlorides, sterically hindered reaction partners, and amides. The practical utility of this micellar system was demonstrated by the gram-scale synthesis of a key pharmaceutical API intermediate and catalyst recycling.
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Chai et al. (2026) studied this question.
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