立体中心
块(置换群论)
试剂
化学
组合化学
克拉斯
碳纤维
计算机科学
对映选择合成
有机化学
数学
算法
生物化学
催化作用
突变
几何学
复合数
基因
作者
Joyce C. Leung,Yibo Xu,Suttipol Radomkit,Jaehee Lee,Wan Shin Kim,Jonathan T. Reeves,Weitong Dong,Hwanjong Jang,Xiaowen Hou,Jon C. Lorenz,Xiao Yu Shao,Denis Byrne,Joe Johnson,Anthony Brundage,Clement Valentin,Phouvieng Beyer,Susan V. DiMeo,Bo Qu,Ruoshi Li,Max Sarvestani,Jinhua J. Song
标识
DOI:10.1021/acs.oprd.3c00362
摘要
Synthesis of molecules containing all-carbon quaternary stereocenters has been a longstanding challenge in organic chemistry. In one of our discovery oncology programs, a key chiral building block bearing an all-carbon quaternary chiral center was of particular interest and was later identified as a core structure for a KRAS G12C inhibitor. Herein, the development of a safer and practical route to the key building block 1 is described. By replacing processes involving the use of an energetic reagent and extensive chromatographic purifications, a scalable process utilizing chemical resolution was developed to access the chiral building block in kilogram quantities, enabling timely delivery of API for preclinical and clinical studies.
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