A commercial
route to adagrasib (1) was developed
to support clinical and commercial needs. Yield was improved to 32%
over six chemical steps. A doubly regioselective SNAr reduced
consumption of a 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.
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