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Abstract
A commercial route to MRTX849 (adagrasib) was developed to support clinical and commercial needs. Yield was improved to 32% over six chemical steps. A doubly regioselective SNAr reduced consumption of an expensive chiral intermediate, reaction optimization led to parts per million palladium catalysis, and a new method to deprotect Cbz-groups were developed to mitigate risk associated with benzyl iodide.
Supplementary materials
Title
Supporting Information
Description
Experimentals and compound characterization
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