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Updated: Jun 15, 2026
Scaled-Up Preparation of an Intermediate of Upatinib, ACT051-3
Published on: April 7, 2023
Improved synthesis of ADAM10 inhibitor GI254023X
Nicole Hoettecke1, Andreas Ludwig, Sabine Foro
1Clemens Schöpf Institute of Chemistry and Biochemistry, Technische Universität Darmstadt, Darmstadt, Germany.
Background:
The metalloproteinases ADAM10 and ADAM17 are involved in various diseases: neurodegeneration, cancer and inflammation.
Objective:
The inhibition of these proteases is a promising target in the treatment of inflammation and cancer.
Methods And Results:
In this study, we present an improved synthesis of the ADAM10 reference inhibitor GI254023X with a higher overall yield, enhanced detection ability and increased acid stability, providing easier handling.
Conclusion:
This upscaled synthesis, free of diastereomeric intermediates, ensures single-batch identity, thus warranting its reproducibility in further biological investigations.
