非对映体
共价键
结晶
化学
再结晶(地质)
立体化学
组合化学
有机化学
生物
古生物学
作者
Xiaogen Yang,Zhiwen Li,Wilsun Xu,Guanming Zhu,Xiantong Feng,Jun Zhang,Hongbin Zhao,Yuyin Chen,Jianshe Kong,Wanping Mai,Lian‐Sheng Li,Daniel J. Pippel,Pingda Ren,Xiaohu Deng
标识
DOI:10.1021/acs.oprd.2c00335
摘要
A scaleup route for a first-generation covalent KRASG12C inhibitor 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.
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