Synthesis of a Highly Functionalized Quinazoline Organozinc toward KRAS G12C Inhibitor <i>Divarasib</i> (GDC-6036), Enabled through Continuous Flow Chemistry-Reference-Cited by-同舟云学术

Synthesis of a Highly Functionalized Quinazoline Organozinc toward KRAS G12C Inhibitor Divarasib (GDC-6036), Enabled through Continuous Flow Chemistry

Published:2023-08-24 Issue: Volume: Page:
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Kelly Sean M.¹^ORCID,Lebl René²,Malig Thomas C.³^ORCID,Bass Thomas M.¹,Kummli Dominique⁴,Kaldre Dainis²,Orcel Ugo²,Tröndlin Lars⁵,Linder David⁵,Sedelmeier Joerg²^ORCID,Bachmann Stephan²,Han Chong¹^ORCID,Zhang Haiming¹^ORCID,Gosselin Francis¹^ORCID

Affiliation:

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

2. Department of Process Chemistry and Catalysis, F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel, Switzerland

3. Department of Small Molecule Analytical Chemistry, Genentech, Inc., South San Francisco, California 94080, United States

4. Department of Solid State Sciences, F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel, Switzerland

5. Department of Drug Substance Scale-up and Supply, F. Hoffmann-La Roche AG, Grenzacherstrasse 124, 4070 Basel, Switzerland

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.3c00164

Reference21 articles.

1. Abstract ND11: Discovery of GDC-6036, a clinical stage treatment for KRAS G12C-positive cancers

2. Targeting KRAS Mutant Cancers with a Covalent G12C-Specific Inhibitor

3. Addressing Atropisomerism in the Development of Sotorasib, a Covalent Inhibitor of KRAS G12C: Structural, Analytical, and Synthetic Considerations

4. Atroposelective Negishi Coupling Optimization Guided by Multivariate Linear Regression Analysis: Asymmetric Synthesis of KRAS G12C Covalent Inhibitor GDC-6036

5. Second-Generation Atroposelective Synthesis of KRAS G12C Covalent Inhibitor GDC-6036

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