Article
Synthesis of Adagrasib (MRTX849), a Covalent KRASG12C Inhibitor Drug for the Treatment of Cancer.
Organic letters - 17 Feb 2023
Chen Cheng-Yi, Lu Zhichao, Scattolin Thomas, Chen Chengsheng, Gan Yonghong, McLaughlin Mark
Abstract excerpt
A concise, transition-metal and protection-free synthesis of adagrasib (MRTX849), a novel KRASG12C inhibitor drug recently approved by the FDA, is reported. Introduction of two chiral building blocks to the tetrahydropyridopyrimidine core was accomplished via two sequential SNAr reactions. Extensive reaction optimization led to a robust, transition-metal-free oxidation of the sulfide intermediate. A judicious...
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