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
Rok vydání:	2023
Předmět:	Organic Chemistry Physical and Theoretical Chemistry
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
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ebe7765e6edfb99a9e83b45071101e9c https://doi.org/10.1021/acs.oprd.2c00386 Zobrazit plný text záznamu