Development of Adagrasib’s Commercial Manufacturing Route
Autor: | David R. Snead, Yonghong Gan, Thomas Scattolin, Dinesh J. Paymode, Michal Achmatowicz, Duane E. Rudisill, Ephraim S. Vidal, Tawfik Gharbaoui, Phil Roberts, Jianbo Yang, Zhangbing Shi, Wei Liu, Joshua Bolger, Zhen Qiao, Cheng-yi Chen |
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Rok vydání: | 2023 |
Předmět: | |
Zdroj: | Organic Process Research & Development. 27:530-538 |
ISSN: | 1520-586X 1083-6160 |
Popis: | 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. |
Databáze: | OpenAIRE |
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