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An expedient, mild and aqueous method for Suzuki–Miyaura diversification of (hetero)aryl halides or (poly)chlorinated pharmaceuticals†‡ † This research work was carried out at the University of St Andrews.‡ Electronic supplementary information (ESI) available. See DOI: 10.1039/d1qo00919b

ABSTRACT: 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 °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. Simple, aqueous and direct cross-coupling of diverse and complex (hetero)aromatic halides and active pharmaceutical agents.

SUBMITTER: Sharma S

PROVIDER: S-EPMC8506956 | biostudies-literature |

REPOSITORIES: biostudies-literature

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