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Tag: Green Discovery Chemistry Award

AstraZeneca

High-throughput Experimentation Enabled Late-stage Functionalization as a Tool for Sustainable Chemistry

High-throughput Experimentation Enabled Late-stage Functionalization as a Tool for Sustainable Chemistry

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.

HTE-enabled Methodology Development and Late-Stage Functionalization for Sustainable Drug Discovery AstraZeneca

Team Members

  • Magnus J. Johansson
  • Daniele Antermite
  • Stig D. Friis
  • Elisa Y. Lai
  • Erik Weis
The winning team consists of Magnus J Johansson, Daniele Antermite, Stig D Friis, Elisa Y Lai and Erik Weis.

More about the Award

The Green Discovery Chemistry Award recognizes outstanding efforts in discovery chemistry that demonstrate compelling environmental, safety, and/or efficiency improvements through green chemistry and engineering. This annual award is presented at the Green Chemistry & Engineering Conference, where a member of the winning team is invited to share their team’s innovations.

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Walk-Up Automated Reaction Profiling (WARP) System: A Tool for Reaction Monitoring Designed for Discovery Chemists

2025 Green Discovery Chemistry Award

The Pfizer team has been awarded the inaugural prize for their submission, “Walk-Up Automated Reaction Profiling (WARP) System: A Tool for Reaction Monitoring Designed for Discovery Chemists.” The WARP system emphasizes waste reduction and minimizing exposure to hazardous substances. The technology provides a useful and versatile profiling tool for challenging reactions and is capable of improving reaction yields, shortening reaction times, and enhancing efficiency in various chemical processes while also reducing environmental impact. It features a simple user interface system to allow open-access use, offering a wide range of options for chemists and expanding the reach of the green chemistry technologies. The winning team consists of Muhammad Alimuddin, John Braganza, Paul Richardson, Wei Wang, and Alex Yanovsky, pictured below.

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