| Autor: |
Yang, Xiaogen, Li, Zhiwen, Xu, Wenwen, Zhu, Guanming, Feng, Xiantong, Zhang, Jun, Zhao, Hongbin, Chen, Yuyin, Kong, Jianshe, Mai, Wanping, Li, Lian-Sheng, Pippel, Daniel J., Ren, Pingda, Deng, Xiaohu |
| Zdroj: |
Organic Process Research & Development; January 2023, Vol. 27 Issue: 1 p206-216, 11p |
| Abstrakt: |
A scaleup route for a first-generation covalent KRASG12Cinhibitor ARS-2102 was devised, featuring an “early cross-coupling” strategy to construct the tetra-substituted atropisomeric biaryl scaffold. An iterative diastereomeric recrystallization enabled an effective chiral resolution of key intermediate 24. A global deprotection followed by chemoselective functionalization afforded ARS-2102 in excellent yield and diastereomeric enrichment. This chromatography-free sequence was successfully executed on kilogram scale. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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