Streamlined Synthesis of SHP2 Inhibitor GDC-1971 Enhanced by a Telescoped Schotten-Baumann SNAr and Reactive Crystallization Cascade

Author:

Sirois Lauren E.1ORCID,White Nicholas A.1ORCID,Shen Jeff1,Dalton Derek M.1ORCID,Zell Daniel1ORCID,St-Jean Frédéric1ORCID,Gosselin Francis1ORCID

Affiliation:

1. Department of Synthetic Molecule Process Chemistry, Genentech, Inc., 1 DNA Way, South San Francisco, California 94080, United States

Publisher

American Chemical Society (ACS)

Reference28 articles.

1. Identification of GDC-1971 (RLY-1971), a SHP2 Inhibitor Designed for the Treatment of Solid Tumors

2. Recent Advances of SHP2 Inhibitors in Cancer Therapy: Current Development and Clinical Application

3. Emerging Therapeutic Approaches of SHP2-Targeted Modulators

4. See reports of ongoing PhI trials at https://www.clinicaltrials.gov; for example:

5. Taylor, A. M.; Lescarbeau, A.; Wang, J.; Zhang, Y.; Lian, G. SHP2 Phosphatase Inhibitors and Methods of Making and Using the Same, U.S. Patent 11,890,281 B2, 2021.

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