Addressing Atropisomerism in the Development of Sotorasib, a Covalent Inhibitor of KRAS G12C: Structural, Analytical, and Synthetic Considerations
Author:
Affiliation:
1. Department of Process Development, Drug Substance Technologies, Amgen Inc., 360 Binney Street, Cambridge, Massachusetts02142, United States
Funder
Amgen
Publisher
American Chemical Society (ACS)
Subject
General Medicine,General Chemistry
Link
https://pubs.acs.org/doi/pdf/10.1021/acs.accounts.2c00479
Reference41 articles.
1. Discovery of a Covalent Inhibitor of KRASG12C (AMG 510) for the Treatment of Solid Tumors
2. Axial Chirality in the Sotorasib Drug Substance, Part 1: Development of a Classical Resolution to Prepare an Atropisomerically Pure Sotorasib Intermediate
3. Axial Chirality in the Sotorasib Drug Substance, Part 2: Leveraging a High-Temperature Thermal Racemization to Recycle the Classical Resolution Waste Stream
4. The Challenge of Atropisomerism in Drug Discovery
5. Assessing Atropisomer Axial Chirality in Drug Discovery and Development
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