Hindered Biaryl Bond Construction and Subsequent Diastereomeric Crystallization to Produce an Atropisomeric Covalent KRAS<sup>G12C</sup> Inhibitor ARS-2102-Reference-Cited by-同舟云学术

Hindered Biaryl Bond Construction and Subsequent Diastereomeric Crystallization to Produce an Atropisomeric Covalent KRAS^G12C Inhibitor ARS-2102

Published:2022-12-28 Issue:1 Volume:27 Page:206-216
ISSN:1083-6160
Container-title:Organic Process Research & Development
language:en
Short-container-title:Org. Process Res. Dev.

Author:

Yang Xiaogen¹,Li Zhiwen¹,Xu Wenwen¹,Zhu Guanming¹,Feng Xiantong²,Zhang Jun²,Zhao Hongbin²,Chen Yuyin²,Kong Jianshe²,Mai Wanping³,Li Lian-Sheng³^ORCID,Pippel Daniel J.⁴,Ren Pingda³,Deng Xiaohu³^ORCID

Affiliation:

1. STA Pharmaceutical Co., Ltd., a WuXi AppTec Company, 288 Fute Zhong Road, Waigaoqiao Pilot Free Trade Zone, Shanghai 200131, China

2. WuXi AppTec Co., Ltd., 168 Nanhai Road, TEDA, Tianjin 300457, China

3. Wellspring Biosciences Inc., 10770 Wateridge Cir. Unit 120, San Diego, California 92121, United States

4. Janssen Research & Development LLC, 3210 Merryfield Row, San Diego, California 92121, United States

Publisher

American Chemical Society (ACS)

Subject

Organic Chemistry,Physical and Theoretical Chemistry

Link

https://pubs.acs.org/doi/pdf/10.1021/acs.oprd.2c00335

Reference33 articles.

1. RAS Proteins and Their Regulators in Human Disease

2. Drugging the undruggable RAS: Mission Possible?

3. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions

4. Direct small-molecule inhibitors of KRAS: from structural insights to mechanism-based design

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