An expedient, mild and aqueous method for Suzuki-Miyaura diversification of (hetero)aryl halides or (poly)chlorinated pharmaceuticals

The development of mild, aqueous conditions for the cross-coupling of highly functionalized (hetero)aryl chlorides or bromides is attractive, enabling their functionalization and diversification. Herein, we report a general method for Suzuki-Miyaura cross-coupling at 37 degrees C in aqueous media in the presence of air. We demonstrate application of this general methodology for derivatisation of (poly)chlorinated, medicinally active compounds and halogenated amino acids. The approach holds the potential to be a useful tool for late-stage functionalization or analogue generation.

Automated summary

The article introduces a method for cross-coupling highly functionalized (hetero)aryl chlorides or bromides under mild, aqueous conditions, and demonstrates its potential for derivatization of medicinally active compounds and halogenated amino acids. This approach could be a useful tool for late-stage functionalization or analogue generation.