2026 Green Discovery Chemistry Award
The AstraZeneca team based in Gothenburg, led by Magnus Johansson, has been recognized for developing a powerful suite of high‑throughput experimentation (HTE)–enabled late‑stage functionalization (LSF) methods that significantly advance sustainable medicinal chemistry. LSF allows direct modification of complex molecules, reducing synthesis steps, protecting‑group use, and overall process mass intensity. By integrating automation, nanomolar-scale miniaturization, and informer libraries, the team minimized waste, solvent consumption, and experimental inefficiency.
Key achievements include cobalt‑catalyzed C–H methylation with benign boron donors, iridium‑catalyzed ortho C–H amination optimized using greener solvents, and ruthenium‑catalyzed C–H amidation enabling rapid linker installation. They also created a meta‑selective C(sp²)–H alkylation platform using sp³‑rich reagents to fine‑tune drug‑like properties. Finally, they shared a unified approach to meta‑methyl and fluoroalkyl drug-like analogues, reducing the number of synthetic steps by up to seven and avoiding PFAS‑classified intermediates.
Together, these integrated HTE‑enabled LSF technologies provide scalable, greener pathways to complex, property‑enhanced molecules while substantially reducing energy use, materials consumption, and hazardous waste.
Team Members
